Filtros de búsqueda

Lista de obras de Craig W Lindsley

"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology

artículo científico publicado en 2011

(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction

artículo científico publicado en 2011

(S)-(+)-Mecamylamine (TC-5214): A Neuronal Nicotinic Receptor Modulator Enters Phase III Trials as an Adjunct Treatment for Major Depressive Disorder (MDD) ⬇️

artículo científico publicado el 18 de agosto de 2010

2012 trends and statistics for prescription medications in the United States: CNS therapeutics continue to hold leading positions

artículo científico publicado en 2013

2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites

artículo científico publicado en 2014

2013 Statistics for global prescription medications: CNS therapeutics maintain a leading position among small molecule therapeutics

artículo científico publicado en 2014

2013 trends and statistics for prescription medications in the United States: CNS highest ranked and record number of prescriptions dispensed

artículo científico publicado en 2015

2015: A New Impact Factor for ACS Chemical Neuroscience and New Topline Data for Global Pharmaceutical Products

artículo científico publicado en 2016

2016: Onward and Upward

artículo científico publicado en 2016

2018: A New Impact Factor and an Expanded Cast of Associate Editors

scientific article published on 01 July 2018

2020-A Year of Growth for ACS Chemical Neuroscience

artículo científico publicado en 2020

2021: A New Year and New Directions for the <i>Journal of Medicinal Chemistry</i>

artículo científico publicado en 2021

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats

artículo científico publicado en 2010

43.1 GENETIC INSIGHTS LEAD TO DISCOVERY OF SELECTIVE ACTIVATORS OF MGLU1 AND MGLU3 METABOTROPIC GLUTAMATE RECEPTORS AS POTENTIAL TREATMENTS FOR SCHIZOPHRENIA.

artículo científico publicado en 2018

A Call to Action on Mental Illness from the World Health Organization.

artículo científico publicado en 2016

A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors

artículo científico publicado en 2014

A General, Enantioselective Synthesis of 1-Azabicyclo[m.n.0]alkane Ring Systems

artículo científico publicado en 2013

A General, Enantioselective Synthesis of Protected Morpholines and Piperazines ⬇️

artículo científico publicado el 22 de mayo de 2012

A New Bromo Trienyne: Synthesis of all-E, Conjugated Tetra-, Penta-, and Hexaenes Common to Oxo Polyene Macrolide Antibiotics ⬇️

artículo científico publicado el 4 de septiembre de 1998

A New Impact Factor and New Directions for ACS Chemical Neuroscience ⬇️

artículo científico publicado el 17 de julio de 2013

A New Impact Factor: the Upward Momentum Continues.

artículo científico publicado en 2014

A Possible Repeal of the Orphan Drug Tax Credit?

artículo científico publicado en 2017

A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo

artículo científico publicado en 2015

A Special “Reviews” Issue on the Chemical Senses.

artículo científico publicado en 2011

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

artículo científico publicado en 2003

A general, enantioselective synthesis of N-alkyl terminal aziridines and C2-functionalized azetidines via organocatalysis

artículo científico publicado en 2015

A general, enantioselective synthesis of β- and γ-fluoroamines

artículo científico publicado en 2013

A new catalytic Cu(II)/sparteine oxidant system for beta,beta-phenolic couplings of styrenyl phenols: synthesis of carpanone and unnatural analogs

scientific article published on 27 August 2008

A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride

artículo científico

A new, non-SSRI mechanism of action for Prozac

artículo científico publicado en 2007

A novel M1 PAM VU0486846 exerts efficacy in cognition models without displaying agonist activity or cholinergic toxicity

artículo científico publicado en 2018

A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin

artículo científico publicado en 2009

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors

artículo científico publicado en 2014

A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies

artículo científico publicado en 2008

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain

artículo científico publicado en 2004

A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning

artículo científico publicado en 2009

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models

artículo científico publicado en 2004

A rodent model of traumatic stress induces lasting sleep and quantitative electroencephalographic disturbances

artículo científico publicado en 2015

A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning

artículo científico publicado en 2009

A unique industrial-academic collaboration towards the next generation of schizophrenia therapeutics

artículo científico

A versatile enantioselective synthesis of azabicyclic ring systems: a concise total synthesis of (+)-grandisine D and unnatural analogues

artículo científico publicado en 2012

ACS Chemical Neuroscience and Neuroscience Drug Discovery as 2012 Comes to a Close ⬇️

artículo científico publicado el 19 de diciembre de 2012

ACS Chemical Neuroscience in 2012:Opportunities and Challenges.

artículo científico publicado en 2012

ACS Chemical Neuroscience in 2014.

artículo científico publicado en 2014

ACS Chemical Neuroscience: Most Cited Papers from 2015.

artículo científico

ACS Chemical Neuroscience: Most Cited Papers from 2016.

artículo científico publicado en 2017

ACS Editors' Choice: Providing Recognition to Authors and Open Access to the Community

artículo científico publicado en 2016

Accelerating Precision Drug Development and Drug Repurposing by Leveraging Human Genetics

artículo científico publicado en 2017

Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus

artículo científico publicado en 2015

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

artículo científico publicado en 2008

Acute Negative Allosteric Modulation of M5 Muscarinic Acetylcholine Receptors Inhibits Oxycodone Self-Administration and Cue-Induced Reactivity with No Effect on Antinociception

scientific article published on 24 July 2019

Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators

artículo científico publicado en 2015

Akt-dependent and isoform-specific regulation of dopamine transporter cell surface expression.

artículo científico publicado en 2010

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors

artículo científico publicado en 2005

Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice.

artículo científico publicado en 2015

Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders

artículo científico publicado en 2013

Allosteric modulation of kinases and GPCRs: design principles and structural diversity

artículo científico publicado en 2008

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

artículo científico publicado en 2012

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

artículo científico publicado en 2013

Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks

artículo científico publicado en 2013

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

artículo científico publicado en 2009

Alzheimer's disease: development of disease-modifying treatments is the challenge for our generation

artículo científico publicado en 2012

An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia

artículo científico publicado en 2016

Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models

artículo científico publicado en 2018

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100

artículo científico publicado en 2014

Antipsychotic-like Effects of M4 Positive Allosteric Modulators Are Mediated by CB2 Receptor-Dependent Inhibition of Dopamine Release

artículo científico publicado en 2016

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)

artículo científico publicado en 2015

Application of combinatorial chemistry science on modern drug discovery

artículo científico publicado en 2008

Applications of microwave-assisted organic synthesis on the multigram scale

artículo científico publicado en 2005

Asymmetric Synthesis of Natural and Unnatural Dibenzylbutane Lignans from a Common Intermediate

scientific article published on 24 April 2019

Attenuation of cocaine's reinforcing and discriminative stimulus effects via muscarinic M1 acetylcholine receptor stimulation.

artículo científico publicado en 2009

Autoregulation of phospholipase D activity is coupled to selective induction of phospholipase D1 expression to promote invasion of breast cancer cells

artículo científico publicado en 2011

Biased M1 receptor-positive allosteric modulators reveal role of phospholipase D in M1-dependent rodent cortical plasticity

scientific article published on 03 December 2019

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents

artículo científico publicado en 2015

Biomimetic Synthesis and Biological Evaluation of Aplidiopsamine A ⬇️

artículo científico publicado el 29 de octubre de 2012

Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism

artículo científico publicado en 2013

CNS Pathogens: A Special Issue of ACS Chemical Neuroscience

artículo científico publicado en 2020

Call for Papers! A SpecialThematic Compilation/Special Issue Crossover with the Journal of Medicinal Chemistry and ACS Medicinal Chemistry Letters Focused on Alzheimer’s Disease.

artículo científico publicado en 2012

Call for Papers: Allosteric Modulators of Drug Targets-Special Issue for 2019

artículo científico publicado en 2018

Call for Papers: DARK Classics in Chemical Neuroscience

artículo científico publicado en 2017

Call for Papers: Strategies and Tactics in CNS Drug Synthesis

scientific article published on 01 March 2019

Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats

artículo científico publicado en 2008

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

artículo científico publicado en 2016

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

artículo científico publicado en 2017

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

artículo científico publicado en 2006

Chemical Modification of the M1 Agonist VU0364572 Reveals Molecular Switches in Pharmacology and a Bitopic Binding Mode ⬇️

artículo científico publicado el 9 de septiembre de 2012

Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death

artículo científico publicado en 2015

Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

artículo científico publicado en 2009

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM

artículo científico publicado en 2010

Chemical modulation of glycerolipid signaling and metabolic pathways

artículo científico

Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics

artículo científico publicado en 2014

Cholinergic Projections to the Substantia Nigra Pars Reticulata Inhibit Dopamine Modulation of Basal Ganglia through the M4 Muscarinic Receptor

artículo científico publicado en 2017

Chronic Traumatic Encephalopathy (CTE): A Brief Historical Overview and Recent Focus on NFL Players

artículo científico publicado en 2017

Chronic Traumatic Encephalopathy (CTE): A Virtual Issue Dedicated to Advances in Understanding, Diagnosing, and Potentially Treating Tauopathies

artículo científico publicado en 2020

Classics in Chemical Neuroscience: Memantine

artículo científico publicado en 2017

Classics in Chemical Neuroscience: Risperidone

artículo científico publicado en 2018

Classics in Chemical Neuroscience: Xanomeline

artículo científico publicado en 2017

Classics in chemical neuroscience: clozapine

artículo científico publicado en 2013

Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP, Long-Term Potentiation, and Disrupts Memory Reconsolidation

artículo científico publicado en 2017

Competition and allostery govern substrate selectivity of cyclooxygenase-2.

artículo científico publicado en 2015

Confronting Racism in Chemistry Journals

scientific article published on 19 June 2020

Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5.

artículo científico publicado en 2017

Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies

artículo científico publicado en 2017

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor ⬇️

artículo científico publicado el 29 de marzo de 2012

Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice ⬇️

artículo científico publicado el 1 de octubre de 2011

Contributions of Protease-Activated Receptors PAR1 and PAR4 to Thrombin-Induced GPIIbIIIa Activation in Human Platelets

artículo científico publicado en 2016

Cooperative signaling between Slit2 and Ephrin-A1 regulates a balance between angiogenesis and angiostasis.

artículo científico publicado en 2010

Correction to Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models

scientific article published on 26 March 2019

Corrigendum: Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders

scholarly article published in Frontiers in molecular neuroscience

Crystal structure of the M5 muscarinic acetylcholine receptor

scientific article published on 26 November 2019

DARK Classics in Chemical Neuroscience: Gamma-Hydroxybutyrate (GHB)

scientific article published on 23 July 2019

DARK Classics in Chemical Neuroscience: Opium, a Historical Perspective

artículo científico publicado en 2018

DARK Classics in Chemical Neuroscience: Phencyclidine (PCP)

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

artículo científico publicado en 2017

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core

artículo científico publicado en 2017

Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity

artículo científico publicado en 2009

Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity

artículo científico publicado en 2009

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.

artículo científico publicado en 2015

Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness

artículo científico publicado en 2009

Design of potent GlyT1 inhibitors: in vitro and in vivo profiles

artículo científico publicado en 2008

Design, Synthesis, and Biological Evaluation of Halogenated N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: Discovery of an Isoform-Selective Small Molecule Phospholipase D2 Inhibitor ⬇️

artículo científico publicado el 23 de septiembre de 2010

Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist

artículo científico publicado en 2008

Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.

artículo científico publicado en 2011

Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides

artículo científico publicado en 2006

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers

artículo científico publicado en 2016

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type

artículo científico publicado en 2015

Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin

artículo científico publicado en 2016

Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries

artículo científico publicado en 2003

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

artículo científico publicado en 2014

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

artículo científico publicado en 2011

Development of a more highly selective M1 antagonist from the continued optimization of the MLPCN Probe ML012 ⬇️

artículo científico publicado el 6 de diciembre de 2011

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.

artículo científico publicado en 2012

Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel

artículo científico publicado en 2010

Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere ⬇️

artículo científico publicado el 24 de noviembre de 2012

Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.

artículo científico publicado en 2013

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012 ⬇️

artículo científico publicado el 15 de junio de 2012

Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity

artículo científico publicado en 2007

Difference in mGluR5 interaction between positive allosteric modulators from two structural classes

artículo científico publicado en 2003

Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators

artículo científico publicado en 2018

Differential effects of allosteric M(1) muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor downregulation

artículo científico publicado en 2010

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor

scientific article published on 04 September 2013

Discoidin domain receptor 1 kinase activity is required for regulating collagen IV synthesis

artículo científico publicado en 2016

Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity

artículo científico publicado en 2014

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

artículo científico publicado en 2018

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

artículo científico publicado en 2009

Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators ⬇️

artículo científico publicado el 18 de julio de 2013

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

artículo científico publicado en 2014

Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold ⬇️

artículo científico publicado el 23 de octubre de 2012

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition

artículo científico

Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators

artículo científico publicado en 2014

Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype

artículo científico

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).

artículo científico publicado en 2015

Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1.

artículo científico publicado en 2014

Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

artículo científico publicado en 2016

Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity

artículo científico publicado en 2008

Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system

artículo científico publicado en 2010

Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe

artículo científico publicado en 2009

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

artículo científico

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): The development of ML169, an MLPCN probe ⬇️

artículo científico publicado el 9 de diciembre de 2010

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM)

artículo científico publicado en 2013

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

artículo científico publicado en 2014

Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels

artículo científico publicado en 2008

Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors

artículo científico publicado en 2005

Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound

artículo científico publicado en 2012

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

artículo científico publicado en 2016

Discovery of GlyT1 inhibitors with improved pharmacokinetic properties

artículo científico publicado en 2009

Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics

artículo científico publicado en 2017

Discovery of ML326: The first sub-micromolar, selective M5 PAM

artículo científico publicado en 2013

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

artículo científico publicado en 2012

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

artículo científico publicado en 2017

Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity

artículo científico publicado en 2010

Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors

artículo científico publicado en 2009

Discovery of Small-Molecule Nonfluorescent Inhibitors of Fluorogen-Fluorogen Activating Protein Binding Pair

artículo científico publicado en 2016

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators

scientific article published on 09 August 2018

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

artículo científico publicado en 2013

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia

artículo científico publicado en 2015

Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

artículo científico publicado en 2014

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

artículo científico publicado en 2016

Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines

artículo científico publicado en 2017

Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology

artículo científico publicado en 2010

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-di

artículo científico publicado en 2017

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

artículo científico publicado en 2015

Discovery of a highly selective PLD2 inhibitor (ML395): a new probe with improved physiochemical properties and broad-spectrum antiviral activity against influenza strains

artículo científico publicado en 2014

Discovery of a new molecular probe ML228: An activator of the hypoxia inducible factor (HIF) pathway ⬇️

artículo científico publicado el 28 de noviembre de 2011

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping

artículo científico publicado en 2017

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core

artículo científico publicado en 2017

Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: Development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia ⬇️

artículo científico publicado el 1 de enero de 2013

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU60

artículo científico publicado en 2019

Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes

artículo científico publicado en 2014

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

artículo científico publicado en 2017

Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines

artículo científico publicado en 2009

Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists ⬇️

artículo científico publicado el 3 de diciembre de 2010

Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity

artículo científico publicado en 2010

Discovery of novel central nervous system penetrant metabotropic glutamate receptor subtype 2 (mGlu) Negative Allosteric Modulators (NAMs) based on functionalized pyrazolo[1,5- a]pyrimidine-5-carboxamide and thieno[3,2- b]pyridine-5-carboxamide cores

article

Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo

artículo científico publicado en 2004

Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).

artículo científico publicado en 2005

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)

artículo científico publicado en 2013

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins

artículo científico publicado en 2009

Discovery of ‘molecular switches’ within a GIRK activator scaffold that afford selective GIRK inhibitors ⬇️

artículo científico publicado el 20 de junio de 2013

Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor

scientific article published on 10 October 2018

Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).

artículo científico publicado en 2016

Discovery, Synthesis, and Structure–Activity Relationship of a Series of N -Aryl-bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener

artículo científico publicado en 2011

Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists

artículo científico publicado en 2016

Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.

artículo científico publicado en 2008

Discovery, characterization, and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.x, and Kir7.1.

artículo científico publicado en 2011

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe

artículo científico publicado en 2014

Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats

artículo científico publicado en 2011

Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate recept

artículo científico publicado en 2011

Discovery, synthesis, and structure-based optimization of a series of N-(tert-butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus [...]

artículo científico publicado en 2013

Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model

artículo científico publicado en 2017

Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs

artículo científico publicado en 2016

Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels ⬇️

artículo científico publicado el 6 de mayo de 2013

Dysregulation of the norepinephrine transporter sustains cortical hypodopaminergia and schizophrenia-like behaviors in neuronal rictor null mice

artículo científico publicado en 2010

Editors' Favorites of 2016.

artículo científico publicado en 2017

Editors' Favorites of 2017.

artículo científico publicado en 2018

Editors' Favorites: Best of 2018

artículo científico publicado en 2019

Effects of VU0410120, a novel GlyT1 inhibitor, on measures of sociability, cognition and stereotypic behaviors in a mouse model of autism

artículo científico publicado en 2015

Efficient synthesis of imidazoles from aldehydes and 1,2-diketones using microwave irradiation

scientific article published on 01 April 2004

Elevating standards for discoveries reported in ACS Chemical Neuroscience: new criteria to enhance reproducibility, experimental transparency, reliability, and the value of negative data

artículo científico publicado en 2014

Embarking on a 5 Year Journey to Highlight Genetic and Rare Diseases of the Central Nervous System

artículo científico publicado en 2017

Emerging Data Strengthens the Argument That the Microbiome Is the Fifth Horseman of the Drug Discovery Apocalypse

artículo científico publicado en 2017

Emerging from the shadow of Vioxx

scientific article published on 01 January 2007

Enantioselective Total Synthesis of (+)-Amabiline ⬇️

artículo científico publicado el 20 de marzo de 2012

Enantioselective synthesis of C2-functionalized, N-protected morpholines and orthogonally N,N′-protected piperazines via organocatalysis ⬇️

artículo científico publicado el 29 de diciembre de 2011

Evaluating the Disposition of a Mixed Aldehyde Oxidase/Cytochrome P450 Substrate in Rats with Attenuated P450 Activity

artículo científico publicado en 2016

Evaluation of the biosynthetic proposal for the synthesis of marineosins A and B

scientific article published on 01 March 2010

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolin

artículo científico publicado en 2013

FAREWELL

artículo científico publicado en 2020

Feeling Rejected? ACS Chemical Neuroscience Can Help Get Your Science to the Neuroscience Community As Quickly As Possible

artículo científico publicado en 2017

Formal Total Synthesis of Pericoannosin A

artículo científico publicado en 2019

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.

artículo científico publicado en 2011

Further evaluation of novel structural modifications to scaffolds that engender PLD isoform selective inhibition

artículo científico publicado en 2014

Further exploration of M1 allosteric agonists: Subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism ⬇️

artículo científico publicado el 9 de noviembre de 2012

Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe ⬇️

artículo científico publicado el 7 de junio de 2012

Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration

artículo científico publicado en 2016

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges

artículo científico publicado en 2014

Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound

artículo científico publicado en 2015

G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms

artículo científico publicado en 2008

General access to chiral N-alkyl terminal aziridines via organocatalysis

artículo científico publicado en 2010

Genetic and Rare Disease of the CNS. Part I: Fatal Familial Insomnia (FFI).

artículo científico publicado en 2017

Genetic and Rare Disease of the CNS. Part II: Holoprosencephaly (HPE)

artículo científico publicado en 2018

GlyT1 − Up from the Ashes. The Importance of Not Condemning a Mechanism Based on a Single Chemotype ⬇️

artículo científico publicado el 17 de marzo de 2010

Glycine transporter-1 inhibition promotes striatal axon sprouting via NMDA receptors in dopamine neurons

artículo científico publicado en 2013

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

artículo científico publicado en 2010

Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions

artículo científico publicado en 2013

High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction

artículo científico publicado en 2014

High-Throughput Screening for Modulators of the D2 Dopamine Receptor Yields Unique and Selective Pharmacological Chemotypes

scholarly article published 2014

High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1.

artículo científico publicado en 2009

Highly Diastereoselective and General Synthesis of Primary β-Fluoroamines ⬇️

artículo científico publicado el 26 de septiembre de 2011

Horner’s Syndrome and Neuroblastoma: Our Family’s Odyssey with Disorders of the Sympathetic Nervous System ⬇️

artículo científico publicado el 20 de octubre de 2010

Human phospholipase D activity transiently regulates pyrimidine biosynthesis in malignant gliomas

artículo científico publicado en 2015

Identification and Characterization of a Compound That Protects Cardiac Tissue from Human Ether-à-go-go-related Gene (hERG)-related Drug-induced Arrhythmias ⬇️

artículo científico publicado el 2 de octubre de 2012

Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter

artículo científico publicado en 2015

Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells.

artículo científico publicado en 2011

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator ⬇️

artículo científico publicado el 2 de agosto de 2012

Identification of ML204, a Novel Potent Antagonist That Selectively Modulates Native TRPC4/C5 Ion Channels ⬇️

artículo científico publicado el 27 de julio de 2011

Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening

artículo científico publicado en 2010

Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding

artículo científico publicado en 2019

Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7

artículo científico publicado en 2014

Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand

artículo científico publicado en 2006

Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site

scientific article published on 26 February 2014

Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles

artículo científico publicado en 2016

Impaired striatal Akt signaling disrupts dopamine homeostasis and increases feeding

artículo científico publicado en 2011

In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.

artículo científico publicado en 2010

Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape ⬇️

artículo científico publicado el 2 de junio de 2011

Inhibition of mammalian target of rapamycin is required for optimal antitumor effect of HER2 inhibitors against HER2-overexpressing cancer cells

artículo científico publicado en 2009

Inhibition of the TRPC5 ion channel protects the kidney filter

artículo científico publicado en 2013

Insulin reveals Akt signaling as a novel regulator of norepinephrine transporter trafficking and norepinephrine homeostasis

artículo científico publicado en 2010

Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships

artículo científico publicado en 2012

Is Zetia a 'do nothing' drug?

artículo científico publicado en 2008

Is the Microbiome the Fifth Horseman of the Apocalypse in Drug Discovery? Implications for the Gut-Brain Axis.

artículo científico publicado en 2017

Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule

artículo científico publicado en 2012

Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma

artículo científico publicado en 2017

Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators

artículo científico publicado en 2012

Label-Free Detection of G Protein–SNARE Interactions and Screening for Small Molecule Modulators ⬇️

artículo científico publicado el 18 de enero de 2012

Lack of Antiparkinsonian Effects of Systemic Injections of the Specific T-Type Calcium Channel Blocker ML218 in MPTP-Treated Monkeys

artículo científico publicado en 2016

Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool

artículo científico publicado en 2016

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core

artículo científico

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs

artículo científico publicado en 2016

Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes

artículo científico publicado en 2016

Loss of Phosphatase and Tensin homologue deleted on chromosome 10 engages ErbB3 and insulin-like growth factor-I receptor signaling to promote antiestrogen resistance in breast cancer

artículo científico publicado en 2009

M-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition

M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons

artículo científico publicado en 2017

M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia

artículo científico publicado en 2015

M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia

article by Weixing Shen et al published 1 June 2016 in Neuron

M4 mAChR-mediated modulation of glutamatergic transmission at corticostriatal synapses

artículo científico publicado en 2014

M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location

artículo científico publicado en 2014

MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines

artículo científico publicado en 2009

ML297 (VU0456810), the First Potent and Selective Activator of the GIRK Potassium Channel, Displays Antiepileptic Properties in Mice ⬇️

artículo científico publicado el 13 de junio de 2013

ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand

artículo científico publicado en 2017

ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels

artículo científico publicado en 2016

Mastering medicinal chemistry: strategies, issues and success stories

artículo científico publicado en 2004

Mechanisms underlying prelimbic prefrontal cortex mGlu/mGlu-dependent plasticity and reversal learning deficits following acute stress

article

Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders

scholarly article by Nicole M Fisher published in January 2018

Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction

artículo científico publicado en 2015

Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature

artículo científico

Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).

artículo científico

Metabotropic glutamate receptor subtype 3 gates acute stress-induced dysregulation of amygdalo-cortical function

artículo científico publicado en 2017

Microplate-based assay for identifying small molecules that bind a specific intersubunit interface within the assembled HIV-1 capsid

artículo científico publicado en 2015

Modulation of pyramidal cell output in the medial prefrontal cortex by mGluR5 interacting with CB1 ⬇️

artículo científico publicado el 6 de abril de 2012

Molecule of the month

artículo científico publicado en 2008

Molecule of the month. FDA approves new treatment for fibromyalgia

artículo científico publicado en 2009

Molecule of the month. Overcoming resistance

artículo científico publicado en 2008

Molecule of the month. The 'skinny' on CB1 antagonists/inverse agonists: controversial obesity drugs will not go to FDA for approval

scientific article published on 01 January 2008

Muscarinic M5 receptors modulate ethanol seeking in rats

artículo científico publicado en 2018

N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats

artículo científico publicado en 2013

N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents

artículo científico publicado en 2016

NeuroChat with Dr. Abdul Mannan Baig

artículo científico publicado en 2020

NeuroChat with Dr. Karen Gregory

artículo científico publicado en 2020

NeuroChat with Dr. Paul A. Newhouse

artículo científico publicado en 2020

NeuroChat with Professor Clinton E. Canal

artículo científico publicado en 2020

NeuroChat with Professor Danny Winder

scientific article published on 01 December 2019

NeuroChat with Professor Kyle Emmitte

scientific article published on 01 January 2020

NeuroChat with Professor P. Jeffrey Conn

scientific article published on 01 January 2020

NeuroChat with Professor Steven Townsend

scientific article published on 01 April 2019

NeuroChat with Professor Thomas E. Prisinzaro

artículo científico publicado en 2020

NeuroChat with Research Assistant Professor Alison Axtman

scientific article published on 01 September 2020

Neuronal ablation of p-Akt at Ser473 leads to altered 5-HT1A/2A receptor function

artículo científico publicado en 2013

New 2016 Data and Statistics for Global Pharmaceutical Products and Projections through 2017.

artículo científico

New 2017 Data and Statistics for Pharmaceutical Products

scientific article published on 01 July 2018

New Hope for Multiple Sclerosis Patients ⬇️

artículo científico publicado el 20 de marzo de 2013

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead

artículo científico publicado en 2014

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres

artículo científico publicado en 2014

Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models

artículo científico publicado en 2012

Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)

artículo científico publicado en 2008

Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats.

artículo científico publicado en 2008

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

artículo científico publicado en 2013

Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

artículo científico publicado en 2014

Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology

artículo científico publicado en 2017

Optimization of a small molecule probe that restores e-cadherin expression

artículo científico publicado en 2015

Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover

artículo científico publicado en 2012

Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound

artículo científico

Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs ⬇️

artículo científico publicado el 1 de septiembre de 2010

PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems

artículo científico publicado en 2018

PLD1 rather than PLD2 regulates phorbol-ester-, adhesion-dependent and Fc{gamma}-receptor-stimulated ROS production in neutrophils

artículo científico publicado en 2011

Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators

artículo científico publicado en 2009

Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects

artículo científico publicado en 2015

Pharmacoeconomics and the medicinal chemist

artículo científico publicado en 2014

Pharmacokinetics, Tissue Localization, Toxicity, and Treatment Efficacy in the First Small Animal (Rabbit) Model of Intra-Arterial Chemotherapy for Retinoblastoma

artículo científico publicado en 2018

Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and L-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist

artículo científico publicado en 2015

Phospholipase D as a Therapeutic Target in Brain Disorders ⬇️

artículo científico publicado el 1 de enero de 2012

Phospholipase D facilitates efficient entry of influenza virus, allowing escape from innate immune inhibition

artículo científico publicado en 2014

Phospholipase D signaling pathways and phosphatidic acid as therapeutic targets in cancer

artículo científico publicado en 2014

Phospholipase D1 Couples CD4+ T Cell Activation to c-Myc-Dependent Deoxyribonucleotide Pool Expansion and HIV-1 Replication

artículo científico publicado en 2015

Phospholipase D2 mediates survival signaling through direct regulation of Akt in glioblastoma cells

artículo científico publicado en 2013

Phospholipase D: enzymology, functionality, and chemical modulation

artículo científico publicado en 2011

Platelet Lipidomic Profiling: Novel Insight into Cytosolic Phospholipase A2α Activity and Its Role in Human Platelet Activation

artículo científico publicado en 2015

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead

artículo científico publicado en 2009

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators

artículo científico publicado en 2008

Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides

scientific article published on 01 September 2006

Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning

artículo científico publicado en 2013

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

artículo científico publicado en 2016

Preclinical drug discovery research and training at Vanderbilt

scientific article published on 01 January 2007

Predictions and Statistics for the Best-Selling Drugs Globally and in the United States in 2018 and a Look Forward to 2024 Projections

scientific article published on 01 March 2019

Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.

artículo científico publicado en 2016

Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia

artículo científico publicado en 2015

Preparation of 1,5-Dihydropyrazolo[3',4':5,6]pyrano[3,4- b]pyridines via a Microwave-Assisted, Palladium-Catalyzed Regioselective C-H Heteroarylation of Electron-Rich Pyrazoles

scientific article published on 07 March 2019

Preparation of Unsymmetrical 1,2,4,5-Tetrazines via a Mild Suzuki Cross-Coupling Reaction

artículo científico publicado en 2017

Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology

artículo científico publicado en 2013

Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors

artículo científico publicado en 2006

Progress toward the total synthesis of lucentamycin A: total synthesis and biological evaluation of 8-epi-lucentamycin A.

artículo científico publicado en 2009

Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility

artículo científico publicado en 2015

Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia

artículo científico publicado en 2006

ROMK inhibitor actions in the nephron probed with diuretics

artículo científico publicado en 2015

Rapid, general access to chiral beta-fluoroamines and beta,beta-difluoroamines via organocatalysis

artículo científico publicado en 2009

Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4

artículo científico publicado en 2010

Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

artículo científico publicado en 2016

Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics ⬇️

artículo científico publicado el 14 de junio de 2011

Recent advances in positive allosteric modulators of metabotropic glutamate receptors

artículo científico publicado en 2005

Recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors

artículo científico publicado en 2007

Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease.

artículo científico publicado en 2009

Recent progress in the discovery and development of negative allosteric modulators of mGluR5.

artículo científico publicado en 2009

Reflections on 2016 and Projecting Forward

artículo científico publicado en 2017

Regulation of Phospholipase D Activity and Phosphatidic Acid Production after Purinergic (P2Y6) Receptor Stimulation ⬇️

artículo científico publicado el 30 de mayo de 2013

Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles

artículo científico publicado en 2014

Restoring Agonist Function at a Chemogenetically Modified M1 Muscarinic Acetylcholine Receptor

artículo científico publicado en 2020

Return of D4 Dopamine Receptor Antagonists in Drug Discovery

artículo científico publicado en 2017

Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay

artículo científico publicado en 2013

Role of mGlu5 Receptors and Inhibitory Neurotransmission in M1 Dependent Muscarinic LTD in the Prefrontal Cortex: Implications in Schizophrenia

artículo científico publicado en 2017

Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson's disease.

artículo científico publicado en 2011

Schizophrenia: moving beyond monoamine antagonists

artículo científico publicado en 2008

Screening and Beyond: New Opportunities to Advance Neuroscience Discovery ⬇️

artículo científico publicado el 17 de febrero de 2010

Selective Inhibition of the Kir2 Family of Inward Rectifier Potassium Channels by a Small Molecule Probe: The Discovery, SAR, and Pharmacological Characterization of ML133 ⬇️

artículo científico publicado el 13 de junio de 2011

Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents

artículo científico publicado en 2014

Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation

artículo científico publicado en 2009

Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats

artículo científico publicado en 2017

Small molecule protein-protein inhibitors for the p53-MDM2 interaction

artículo científico publicado en 2007

Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition

artículo científico publicado en 2015

Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2

artículo científico publicado en 2009

Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.

artículo científico publicado en 2011

Special issue on the pharmacology and medicinal chemistry of allosteric modulators of metabotropic glutamate receptors (mGluRs).

artículo científico publicado en 2011

Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant).

artículo científico publicado en 2017

Specific activin receptor-like kinase 3 inhibitors enhance liver regeneration

artículo científico publicado en 2014

Spiroaminal model systems of the marineosins with final step pyrrole incorporation ⬇️

artículo científico publicado el 1 de mayo de 2013

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule

artículo científico publicado en 2013

State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects

artículo científico publicado en 2015

Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallogr

artículo científico publicado en 2018

Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae

scientific article published on 30 November 2018

Structure-Activity Relationships of Pan-Gα Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction

artículo científico publicado en 2013

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

artículo científico publicado en 2014

Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders

artículo científico publicado en 2009

Synthesis and Biological Evaluation of Cremastrine and an Unnatural Analogue

artículo científico publicado en 2012

Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides

artículo científico publicado en 2006

Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists

artículo científico publicado en 2010

Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

artículo científico publicado en 2008

Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: Unexpected ‘molecular switch’ from a closely related mGlu4 positive allosteric modulator ⬇️

artículo científico publicado el 8 de octubre de 2011

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).

artículo científico publicado en 2009

Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen

artículo científico publicado en 2008

Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties

artículo científico publicado en 2008

Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold ⬇️

artículo científico publicado el 18 de enero de 2011

Synthesis and SAR of novel histamine H3 receptor antagonists

artículo científico publicado en 2006

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).

artículo científico publicado en 2010

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

artículo científico

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists

artículo científico publicado en 2008

Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs

artículo científico publicado en 2014

Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists ⬇️

artículo científico publicado el 23 de septiembre de 2012

Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists

artículo científico publicado en 2016

Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype

artículo científico publicado en 2017

Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

artículo científico publicado en 2009

Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter

artículo científico publicado en 2015

Synthesis and structure-activity relationships of allosteric potentiators of the m(4) muscarinic acetylcholine receptor

artículo científico publicado en 2009

Synthesis of 2,3-diarylsubstituted indazoles utilizing a Suzuki cross-coupling/deprotection/N-arylation sequence

artículo científico publicado en 2010

Synthesis of Indole Derived Protease-Activated Receptor 4 Antagonists and Characterization in Human Platelets ⬇️

artículo científico publicado el 11 de junio de 2013

Synthesis of Substituted 6,7-Dihydro-5H-pyrrolo[2,3-c]pyridazines/pyrazines via Catalyst-Free Tandem Hydroamination-Aromatic Substitution

artículo científico publicado en 2020

Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273

artículo científico publicado en 2009

T227. THE METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE 1 REGULATES STRIATAL DOPAMINE RELEASE VIA AN ENDOCANNABINOID-DEPENDENT MECHANISM: IMPLICATIONS FOR THE TREATMENT OF SCHIZOPHRENIA.

artículo científico publicado en 2018

T39. NEURAL MECHANISMS OF METABOTROPIC GLUTAMATE RECEPTOR 3 MEDIATED ENHANCEMENT OF SYNAPTIC PLASTICITY AND COGNITION.

artículo científico publicado en 2018

Targeting phospholipase D in cancer, infection and neurodegenerative disorders

artículo científico publicado en 2017

Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.

artículo científico publicado en 2012

Targeting the phosphatidylinositol-3 kinase/Akt pathway for the treatment of cancer

artículo científico publicado en 2005

Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).

artículo científico publicado en 2014

The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation

artículo científico publicado en 2005

The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation: a 2009 update

artículo científico publicado en 2010

The Akt/PKB pathway: molecular target for cancer drug discovery

artículo científico publicado en 2005

The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

artículo científico publicado en 2011

The Ecstasy and Agony of Assay Interference Compounds

artículo científico publicado en 2017

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

artículo científico publicado en 2017

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

scientific article published in 2017

The Ecstasy and Agony of Assay Interference Compounds

artículo científico publicado en 2017

The Ecstasy and Agony of Assay Interference Compounds.

artículo científico publicado en 2017

The Evolution of Histamine H3 Antagonists/Inverse Agonists ⬇️

artículo científico publicado el 1 de enero de 2011

The Last Issue of Our Inaugural Year: Reflections and a View to the Future.

artículo científico publicado en 2010

The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation

scientific article published on 17 October 2018

The NIH's role in accelerating translational sciences ⬇️

artículo científico publicado el 9 de enero de 2012

The PI3K/Akt pathway: recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors

artículo científico publicado en 2008

The Top Prescription Drugs of 2010 in the United States: Antipsychotics Show Strong Growth ⬇️

artículo científico publicado el 15 de junio de 2011

The antipsychotic potential of muscarinic allosteric modulation

artículo científico publicado en 2010

The end of an era and new beginnings for the editorial leadership of ACS Chemical Neuroscience

artículo científico publicado en 2013

The future of neurodegenerative diseases: emerging targets, treatments and technologies

artículo científico publicado en 2012

The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.

artículo científico publicado en 2011

The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.

artículo científico publicado en 2012

The synthesis and preclinical evaluation in rhesus monkey of [18F]MK‐6577 and [11C]CMPyPB glycine transporter 1 positron emission tomography radiotracers ⬇️

artículo científico publicado el 1 de abril de 2011

The top prescription drugs of 2009 in the US: CNS therapeutics rank among highest grossing

artículo científico publicado en 2010

The top prescription drugs of 2011 in the United States: antipsychotics and antidepressants once again lead CNS therapeutics

artículo científico publicado en 2012

The top prescription drugs of 2012 globally: biologics dominate, but small molecule CNS drugs hold on to top spots

artículo científico publicado en 2013

Torn from the Headlines: Angiostrongylus cantonensis (Rat Lungworm) Is Established in Florida

artículo científico publicado en 2017

Torn from the Headlines: Surviving the "Brain Eating Amoeba".

artículo científico publicado en 2016

Torn from the headlines: AstraZeneca fined for illegal marketing of SEROQUEL.

artículo científico publicado en 2010

Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target

artículo científico publicado en 2018

Total Synthesis and Biological Evaluation of Hybrubin A.

artículo científico publicado en 2016

Total Synthesis and Biological Evaluation of Phidianidines A and B Uncovers Unique Pharmacological Profiles at CNS Targets ⬇️

artículo científico publicado el 27 de junio de 2012

Total Synthesis of (+)-7-Bromotrypargine and Unnatural Analogues: Biological Evaluation Uncovers Activity at CNS Targets of Therapeutic Relevance ⬇️

artículo científico publicado el 16 de noviembre de 2011

Total Synthesis of Hinduchelins A-D, Stereochemical Revision of Hinduchelin A, and Biological Evaluation of Natural and Unnatural Analogues

artículo científico publicado en 2019

Total Synthesis of Stemaphylline N‐Oxide and Related C9a‐Epimeric Analogues ⬇️

artículo científico publicado el 16 de agosto de 2013

Total synthesis and biological evaluation of tambjamine K and a library of unnatural analogs

artículo científico publicado en 2010

Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential

artículo científico publicado en 2008

Total synthesis of Ciliatamides A-C: stereochemical revision and the natural product-guided synthesis of unnatural analogs

artículo científico publicado en 2008

Total synthesis of brevisamide

artículo científico publicado en 2009

Towards the Total Synthesis of Marineosin A: Construction of the Macrocyclic Pyrrole and an Advanced, Functionalized Spiroaminal Model

artículo científico publicado en 2013

Towards the treatment of Alzheimer's disease: Discovery and development of novel subtype-specific M1 allosteric agonists

article

Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members

artículo científico publicado en 2005

Tumor necrosis factor (TNF) blockers ignite FDA inquiry over cancer concerns

artículo científico publicado en 2008

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity

artículo científico publicado en 2012

Update to Our Reader, Reviewer, and Author Communities-April 2020

scientific article published on 22 April 2020

Update to Our Reader, Reviewer, and Author Communities-April 2020

artículo científico publicado en 2020

Use of chemical probes to explore the toxicological potential of the K/Cl cotransporter (KCC) as a novel insecticide target to control the primary vector of dengue and Zika virus, Aedes aegypti

artículo científico publicado en 2018

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy

artículo científico publicado en 2015

Web enabling technology for the design, enumeration, optimization and tracking of compound libraries

artículo científico publicado en 2005

Welcome to Professor Hsin-Yi Lai, the Newest Associate Editor for ACS Chemical Neuroscience

artículo científico publicado en 2020

Welcome to the DARK Side: DARK Classics in Chemical Neuroscience

artículo científico publicado en 2018

What Papers Are People Citing and What Are People Reading?

scientific article published on 01 September 2018

Yohimbine Depresses Excitatory Transmission in BNST and Impairs Extinction of Cocaine Place Preference Through Orexin-Dependent, Norepinephrine-Independent Processes.

artículo científico publicado en 2013

Yohimbine depresses excitatory transmission in BNST and impairs extinction of cocaine place preference through orexin-dependent, norepinephrine-independent processes ⬇️

artículo científico publicado en 2012

cFLIP critically modulates apoptotic resistance in epithelial-to-mesenchymal transition

artículo científico publicado en 2017

mGlu1 and mGlu5 modulate distinct excitatory inputs to the nucleus accumbens shell

artículo científico publicado en 2018

mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome

artículo científico publicado en 2016

mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome.

artículo científico publicado en 2017

mGluR4-positive allosteric modulation as potential treatment for Parkinson's disease.

artículo científico publicado en 2009

mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning

artículo científico publicado en 2009

Dominio Público Uruguay está sostenido por:

Acerca de Dominio Público Uruguay

Ayuda