Lista de obras - John Atack - Dominio Público Uruguay

2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.

artículo científico publicado en 2006

3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.

artículo científico publicado en 2004

3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.

artículo científico publicado en 2002

3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.

artículo científico publicado en 2004

6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.

artículo científico publicado en 2002

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic

artículo científico publicado en 2005

A Biophysical Approach to the Identification of Novel ApoE Chemical Probes

scientific article published on 29 January 2019

A neural tube defect specific form of acetylcholinesterase in amniotic fluid

scientific article published on 01 December 1983

A new pyridazine series of GABAA alpha5 ligands.

artículo científico publicado en 2005

Absence of biochemical heterogeneity in McArdle's disease. A high resolution SDS-polyacrylamide gel electrophoresis study

artículo científico publicado en 1987

African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase

artículo científico publicado en 2017

Alpha2-containing GABA(A) receptors are involved in mediating stimulant effects of cocaine.

artículo científico publicado en 2008

Aluminosilicates and senile plaque formation in Alzheimer's disease.

artículo científico publicado en 1986

An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.

artículo científico publicado en 2005

An inverse agonist selective for alpha5 subunit-containing GABAA receptors improves encoding and recall but not consolidation in the Morris water maze.

artículo científico publicado en 2006

An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.

artículo científico publicado en 2004

Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site

artículo científico publicado en 2003

Bilateral changes in neocortical [3H]pirenzepine and [3H]oxotremorine-M binding following unilateral lesions of the rat nucleus basalis magnocellularis: an autoradiographic study

artículo científico publicado en 1989

Carbamate analogues of (-)-physostigmine: in vitro inhibition of acetyl- and butyrylcholinesterase

artículo científico publicado en 1988

Cell surface expression of the human N-methyl-D-aspartate receptor subunit 1a requires the co-expression of the NR2A subunit in transfected cells.

artículo científico publicado en 1996

Cerebrospinal fluid cholinesterases in aging and in dementia of the Alzheimer type

scientific article published on 01 February 1988

Cerebrospinal fluid inositol monophosphatase: elevated activity in depression and neuroleptic-treated schizophrenia

artículo científico publicado en 1998

Cerebrospinal fluid neurochemistry in the myoclonic subtype of Alzheimer's disease

scientific article published on 01 November 1988

Cerebrospinal fluid production is normal in Down syndrome ⬇️

artículo científico publicado el 1 de julio de 1998

Changes in [3H]zolpidem and [3H]Ro 15-1788 binding in rat globus pallidus and substantia nigra pars reticulata following a nigrostriatal tract lesion

scientific article published on 01 April 2000

Characterization of [35S]t-butylbicyclophosphorothionate ([35S]TBPS) binding to GABAA receptors in postmortem human brain

artículo científico publicado en 2007

Characterization of inositol monophosphatase in human cerebrospinal fluid.

artículo científico publicado en 1993

Characterization of the effects of lithium on phosphatidylinositol (PI) cycle activity in human muscarinic m1 receptor-transfected CHO cells.

artículo científico publicado en 1993

Cholinergic correlates of cognitive impairment in Parkinson's disease: comparisons with Alzheimer's disease.

artículo científico publicado en 1985

Co-crystallization of human inositol monophosphatase with the lithium mimetic L-690,330

artículo científico publicado en 2018

Cocaine effects on mouse incentive-learning and human addiction are linked to alpha2 subunit-containing GABAA receptors

artículo científico publicado en 2010

Combining Sanford Arylations on Benzodiazepines with the Nuisance Effect

artículo científico publicado en 2017

Comparison of lorazepam [7-chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one] occupancy of rat brain gamma-aminobutyric acid(A) receptors measured using in vivo [3H]flumazenil (8-fluoro 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[

artículo científico publicado en 2006

Contribution of GABAA receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys ⬇️

artículo científico publicado el 30 de diciembre de 2010

Contribution of specific binding to the central benzodiazepine site to the brain concentrations of two novel benzodiazepine site ligands.

artículo científico publicado en 2007

Crystallization and structure of ebselen bound to Cys141 of human inositol monophosphatase

scientific article published on 15 September 2020

Decreased CSF inositol monophosphatase activity after lithium treatment.

artículo científico publicado en 1994

Detection of gender differences in rat lens proteins using 2-D-DIGE.

artículo científico publicado en 2006

Development of an oligonucleotide-based fluorescence assay for the identification of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors.

artículo científico publicado en 2014

Different GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates

artículo científico publicado en 2005

Differential contribution of GABA(A) receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands.

artículo científico publicado en 2006

Differential expression of cytochrome oxidase (COX) genes in different regions of monkey brain

artículo científico publicado el 1 de julio de 1992

Discovery of Imidazo[1,2-b][1,2,4]triazines as GABAAα2/3 Subtype Selective Agonists for the Treatment of Anxiety

article

Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux.

artículo científico publicado en 2001

Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.

artículo científico publicado en 2005

GABA(A) Receptor Subtypes: Novel Targets for Novel Medicines

artículo científico publicado en 2012

GABAA Receptor Subtype-Selective Modulators. II. &#945;5-Selective Inverse Agonists for Cognition Enhancement ⬇️

artículo científico publicado el 1 de enero de 2011

GABAA Receptor α2/α3 Subtype-Selective Modulators as Potential Nonsedating Anxiolytics ⬇️

artículo científico publicado el 1 de enero de 2010

GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics.

artículo científico publicado en 2011

Identification of a Novel, Selective GABAAα5 Receptor Inverse Agonist Which Enhances Cognition ⬇️

artículo científico publicado el 22 de mayo de 2003

Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135)

artículo científico publicado en 2008

Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

artículo científico publicado en 2005

Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

artículo científico publicado en 2006

In vitro and in vivo inhibition of inositol monophosphatase by the bisphosphonate L-690,330.

artículo científico publicado en 1993

In vitro and in vivo inhibition of prolyl endopeptidase ⬇️

artículo científico publicado el 26 de noviembre de 1991

In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist.

artículo científico publicado en 2009

In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat.

artículo científico publicado en 2006

In vivo labelling of alpha5 subunit-containing GABA(A) receptors using the selective radioligand [(3)H]L-655,708.

artículo científico publicado en 2005

Inositol monophosphatase inhibitors: A novel treatment for bipolar disorder? ⬇️

artículo científico publicado el 1 de junio de 1995

Inositol monophosphatase, the putative therapeutic target for lithium

artículo científico publicado en 1996

Interaction of 9-amino-1,2,3,4-tetrahydroaminoacridine (THA) with human cortical nicotinic and muscarinic receptor binding in vitro

scientific article published on 01 August 1988

Intralaminar Neurochemical Distributions in Human Midtemporal Cortex: Comparison Between Alzheimer's Disease and the Normal ⬇️

artículo científico publicado el 1 de mayo de 1984

JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease

artículo científico publicado en 2014

L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for alpha5-containing GABAA receptors.

artículo científico publicado en 2006

Lipophilic nalmefene prodrugs to achieve a one-month sustained release.

artículo científico publicado en 2016

Lumbar cerebrospinal fluid choline in healthy aging and in Down's syndrome.

artículo científico publicado en 1990

MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.

artículo científico publicado en 2010

Mechanism of inositol monophosphatase, the putative target of lithium therapy

artículo científico publicado en 1994

Mode of action of DNA-competitive small molecule inhibitors of tyrosyl DNA phosphodiesterase 2.

artículo científico publicado en 2016

Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor.

artículo científico publicado en 2015

Molecular forms of acetylcholinesterase and butyrylcholinesterase in human plasma and cerebrospinal fluid

artículo científico publicado en 1987

Molecular forms of butyrylcholinesterase in the human neocortex during development and degeneration of the cortical cholinergic system.

artículo científico publicado en 1987

Neural tube defect-specific acetylcholinesterase: its properties and quantitation in the detection of anencephaly and spina bifida

scientific article published on 01 November 1987

Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.

artículo científico publicado en 2010

Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction.

artículo científico publicado en 2005

Pharmacological characterisation of MDI-222, a novel AMPA receptor positive allosteric modulator with an improved safety profile

artículo científico publicado en 2019

Plasma and erythrocyte acetylcholinesterase in senile dementia of Alzheimer type.

artículo científico publicado en 1982

Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.

artículo científico publicado en 2010

Preclinical and clinical pharmacology of the GABAA receptor alpha5 subtype-selective inverse agonist alpha5IA.

artículo científico publicado en 2009

Probing the role of metal ions in the mechanism of inositol monophosphatase by site-directed mutagenesis

scientific article published on 01 October 1993

Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro

artículo científico publicado en 2005

R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization.

artículo científico publicado en 2007

Rat and human hippocampal alpha5 subunit-containing gamma-aminobutyric AcidA receptors have alpha5 beta3 gamma2 pharmacological characteristics.

artículo científico publicado en 1998

Rat pharmacokinetics and pharmacodynamics of a sustained release formulation of the GABAA alpha5-selective compound L-655,708.

artículo científico publicado en 2006

Reducing abuse liability of GABAA/benzodiazepine ligands via selective partial agonist efficacy at alpha1 and alpha2/3 subtypes

artículo científico publicado en 2009

Regional analysis of rat brain proteins during senescence

artículo científico publicado en 1987

Regional differences in the inhibition of mouse in vivo [3H]Ro 15-1788 binding reflect selectivity for alpha 1 versus alpha 2 and alpha 3 subunit-containing GABAA receptors.

artículo científico publicado en 1999

Regional specificity of membrane instability in Alzheimer's disease brain.

artículo científico publicado en 1993

Reinforcing Effects Of Compounds Lacking Intrinsic Efficacy At α1 Subunit-Containing GABAA Receptor Subtypes in Midazolam- But Not Cocaine-Experienced Rhesus Monkeys ⬇️

artículo científico publicado el 27 de diciembre de 2012

Rodent pharmacokinetics and receptor occupancy of the GABAA receptor subtype selective benzodiazepine site ligand L-838417.

artículo científico publicado en 2005

Role of GABAA alpha5-containing receptors in ethanol reward: the effects of targeted gene deletion, and a selective inverse agonist

artículo científico publicado en 2005

Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype.

artículo científico publicado en 2000

Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents.

artículo científico publicado en 2007

Selective labelling of diazepam-insensitive GABAA receptors in vivo using [3H]Ro 15-4513

artículo científico publicado en 2005

Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.

artículo científico publicado en 2004

Structure and mechanism of inositol monophosphatase.

artículo científico publicado en 1995

Structure of inositol monophosphatase, the putative target of lithium therapy ⬇️

artículo científico publicado el 1 de noviembre de 1992

Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour.

artículo científico publicado en 2004

Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.

artículo científico publicado en 2004

TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for alpha2- and alpha3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates.

artículo científico publicado en 2005

The 5HT(1B) receptor agonist, CP-93129, inhibits [(3)H]-GABA release from rat globus pallidus slices and reverses akinesia following intrapallidal injection in the reserpine-treated rat

artículo científico publicado en 2000

The X-ray structure of human calbindin-D28K: an improved model

article

The characterisation of molecular forms of acetylcholinesterase in Hirschsprung's disease ⬇️

artículo científico publicado el 15 de febrero de 1988

The complexity of the GABAA receptor shapes unique pharmacological profiles.

scientific article published on 02 July 2009

The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor

artículo científico publicado en 2011

The in vivo properties of pagoclone in rat are most likely mediated by 5'-hydroxy pagoclone

artículo científico publicado en 2006

The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.

artículo científico publicado en 2006

The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, alpha5IA, is similar in rats and primates

artículo científico publicado en 2009

The proconvulsant effects of the GABAA alpha5 subtype-selective compound RY-080 may not be alpha5-mediated.

artículo científico publicado en 2006

Tyrosine 121 moves revealing a ligandable pocket that couples catalysis to ATP-binding in serine racemase

artículo científico publicado en 2022

cDNA cloning of human and rat brain myo-inositol monophosphatase. Expression and characterization of the human recombinant enzyme ⬇️

artículo científico publicado el 15 de junio de 1992

pp60c-src Kinase expression in brain of adult rats in relation to age ⬇️

artículo científico publicado el 1 de enero de 1990

Lista de obras de John Atack

2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.

3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.

3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.

3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.

6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic

A Biophysical Approach to the Identification of Novel ApoE Chemical Probes

A neural tube defect specific form of acetylcholinesterase in amniotic fluid

A new pyridazine series of GABAA alpha5 ligands.

Absence of biochemical heterogeneity in McArdle's disease. A high resolution SDS-polyacrylamide gel electrophoresis study

African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase

Alpha2-containing GABA(A) receptors are involved in mediating stimulant effects of cocaine.

Aluminosilicates and senile plaque formation in Alzheimer's disease.

An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.

An inverse agonist selective for alpha5 subunit-containing GABAA receptors improves encoding and recall but not consolidation in the Morris water maze.

An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.

Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site

Bilateral changes in neocortical [3H]pirenzepine and [3H]oxotremorine-M binding following unilateral lesions of the rat nucleus basalis magnocellularis: an autoradiographic study

Carbamate analogues of (-)-physostigmine: in vitro inhibition of acetyl- and butyrylcholinesterase

Cell surface expression of the human N-methyl-D-aspartate receptor subunit 1a requires the co-expression of the NR2A subunit in transfected cells.

Cerebrospinal fluid cholinesterases in aging and in dementia of the Alzheimer type

Cerebrospinal fluid inositol monophosphatase: elevated activity in depression and neuroleptic-treated schizophrenia

Cerebrospinal fluid neurochemistry in the myoclonic subtype of Alzheimer's disease

Cerebrospinal fluid production is normal in Down syndrome ⬇️

Changes in [3H]zolpidem and [3H]Ro 15-1788 binding in rat globus pallidus and substantia nigra pars reticulata following a nigrostriatal tract lesion

Characterization of [35S]t-butylbicyclophosphorothionate ([35S]TBPS) binding to GABAA receptors in postmortem human brain

Characterization of inositol monophosphatase in human cerebrospinal fluid.

Characterization of the effects of lithium on phosphatidylinositol (PI) cycle activity in human muscarinic m1 receptor-transfected CHO cells.

Cholinergic correlates of cognitive impairment in Parkinson's disease: comparisons with Alzheimer's disease.

Co-crystallization of human inositol monophosphatase with the lithium mimetic L-690,330

Cocaine effects on mouse incentive-learning and human addiction are linked to alpha2 subunit-containing GABAA receptors

Combining Sanford Arylations on Benzodiazepines with the Nuisance Effect

Comparison of lorazepam [7-chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one] occupancy of rat brain gamma-aminobutyric acid(A) receptors measured using in vivo [3H]flumazenil (8-fluoro 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[

Contribution of GABAA receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys ⬇️

Contribution of specific binding to the central benzodiazepine site to the brain concentrations of two novel benzodiazepine site ligands.

Crystallization and structure of ebselen bound to Cys141 of human inositol monophosphatase

Decreased CSF inositol monophosphatase activity after lithium treatment.

Detection of gender differences in rat lens proteins using 2-D-DIGE.

Development of an oligonucleotide-based fluorescence assay for the identification of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors.

Different GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates

Differential contribution of GABA(A) receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands.

Differential expression of cytochrome oxidase (COX) genes in different regions of monkey brain

Discovery of Imidazo[1,2-b][1,2,4]triazines as GABAAα2/3 Subtype Selective Agonists for the Treatment of Anxiety

Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux.

Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.

GABA(A) Receptor Subtypes: Novel Targets for Novel Medicines

GABAA Receptor Subtype-Selective Modulators. II. &amp;#945;5-Selective Inverse Agonists for Cognition Enhancement ⬇️

GABAA Receptor α2/α3 Subtype-Selective Modulators as Potential Nonsedating Anxiolytics ⬇️

GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics.

Identification of a Novel, Selective GABAAα5 Receptor Inverse Agonist Which Enhances Cognition ⬇️

Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135)

Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

In vitro and in vivo inhibition of inositol monophosphatase by the bisphosphonate L-690,330.

In vitro and in vivo inhibition of prolyl endopeptidase ⬇️

In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist.

In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat.

In vivo labelling of alpha5 subunit-containing GABA(A) receptors using the selective radioligand [(3)H]L-655,708.

Inositol monophosphatase inhibitors: A novel treatment for bipolar disorder? ⬇️

Inositol monophosphatase, the putative therapeutic target for lithium

Interaction of 9-amino-1,2,3,4-tetrahydroaminoacridine (THA) with human cortical nicotinic and muscarinic receptor binding in vitro

Intralaminar Neurochemical Distributions in Human Midtemporal Cortex: Comparison Between Alzheimer's Disease and the Normal ⬇️

JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease

L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for alpha5-containing GABAA receptors.

Lipophilic nalmefene prodrugs to achieve a one-month sustained release.

Lumbar cerebrospinal fluid choline in healthy aging and in Down's syndrome.

MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.

Mechanism of inositol monophosphatase, the putative target of lithium therapy

Mode of action of DNA-competitive small molecule inhibitors of tyrosyl DNA phosphodiesterase 2.

Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor.

Molecular forms of acetylcholinesterase and butyrylcholinesterase in human plasma and cerebrospinal fluid

Molecular forms of butyrylcholinesterase in the human neocortex during development and degeneration of the cortical cholinergic system.

Neural tube defect-specific acetylcholinesterase: its properties and quantitation in the detection of anencephaly and spina bifida

Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.

Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction.

Pharmacological characterisation of MDI-222, a novel AMPA receptor positive allosteric modulator with an improved safety profile

Plasma and erythrocyte acetylcholinesterase in senile dementia of Alzheimer type.

Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.

Preclinical and clinical pharmacology of the GABAA receptor alpha5 subtype-selective inverse agonist alpha5IA.

GABAA Receptor Subtype-Selective Modulators. II. α5-Selective Inverse Agonists for Cognition Enhancement ⬇️