Lista de obras -

1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia ⬇️

artículo científico publicado el 13 de diciembre de 2010

3-Amino-1,5-benzodiazepinones: Potent, state-dependent sodium channel blockers with anti-epileptic activity

article

A novel 3-dimensional micro-ultrasound approach to automated measurement of carotid arterial plaque volume as a biomarker for experimental atherosclerosis

artículo científico publicado en 2008

A role for the melanocortin 4 receptor in sexual function

artículo científico publicado en 2002

Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula

artículo científico publicado en 2002

Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker

artículo científico publicado en 2010

Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents

artículo científico publicado en 2007

Benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain

article

Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.

artículo científico publicado en 2003

Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase

artículo científico publicado en 2005

Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents

artículo científico publicado en 2007

Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats

artículo científico publicado en 2003

Comparison of Cardiovascular Parameters and/or Serum Chemistry and Hematology Profiles in Conscious and Anesthetized Rhesus Monkeys (Macaca mulatta)

artículo científico publicado en 1999

Contribution of the tetrodotoxin-resistant voltage-gated sodium channel NaV1.9 to sensory transmission and nociceptive behavior

artículo científico publicado en 2005

Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR

scientific article published on 07 July 2006

Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives

artículo científico publicado en 2006

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor ago

artículo científico publicado en 2002

Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocorti

artículo científico publicado en 2005

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

artículo científico publicado en 2005

Discovery of a novel class of benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain

article

Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist

artículo científico publicado en 2011

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist

artículo científico publicado en 2010

Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists

artículo científico publicado en 2010

Effects of sildenafil on erectile activity in mice lacking neuronal or endothelial nitric oxide synthase

artículo científico publicado en 2002

Effects of the ventilatory stimulant, doxapram on human TASK-3 (KCNK9, K2P9.1) channels and TASK-1 (KCNK3, K2P3.1) channels

artículo científico publicado en 2019

GAL-021 and GAL-160 are Efficacious in Rat Models of Obstructive and Central Sleep Apnea and Inhibit BKCa in Isolated Rat Carotid Body Glomus Cells ⬇️

artículo científico publicado en 2015

Ghrelin neutralization by a ribonucleic acid-SPM ameliorates obesity in diet-induced obese mice

artículo científico publicado en 2005

Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator

artículo científico publicado en 2015

Identification of glucose-dependant insulin secretion targets in pancreatic beta cells by combining defined-mechanism compound library screening and siRNA gene silencing

scientific journal article

Impaired neuropathic pain responses in mice lacking the chemokine receptor CCR2

scientific journal article

Inhibition of soluble epoxide hydrolase attenuates endothelial dysfunction in animal models of diabetes, obesity and hypertension

scientific article published on 25 December 2010

Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists

artículo científico publicado en 2007

Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism

artículo científico publicado en 2002

Melanocortin receptors and erectile function

artículo científico publicado en 2004

Pharmacokinetics and pharmacodynamics of AR9281, an inhibitor of soluble epoxide hydrolase, in single- and multiple-dose studies in healthy human subjects

scientific article published on 21 March 2011

Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation

artículo científico publicado en 2009

Structure-activity relationship of linear tetrapeptides Tic-DPhe-Arg-Trp-NH2 at the human melanocortin-4 receptor and effects on feeding behaviors in rat.

artículo científico publicado en 2005

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators

artículo científico publicado en 2008

Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

artículo científico publicado en 2005

The proof of the pudding is in the eating: editorial focus on "Hyperphagia, not hypometabolism, causes early onset obesity in melanocortin-4-receptor knockout mice"

artículo científico publicado en 2003

The role of melanocortins in body weight regulation: opportunities for the treatment of obesity

artículo científico publicado en 2002

The role of melanocortins in body weight regulation: opportunities for the treatment of obesity

artículo científico publicado en 2002

The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)

scientific journal article

Lista de obras de

1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia ⬇️

3-Amino-1,5-benzodiazepinones: Potent, state-dependent sodium channel blockers with anti-epileptic activity

A novel 3-dimensional micro-ultrasound approach to automated measurement of carotid arterial plaque volume as a biomarker for experimental atherosclerosis

A role for the melanocortin 4 receptor in sexual function

Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula

Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker

Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents

Benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain

Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.

Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase

Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents

Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats

Comparison of Cardiovascular Parameters and/or Serum Chemistry and Hematology Profiles in Conscious and Anesthetized Rhesus Monkeys (Macaca mulatta)

Contribution of the tetrodotoxin-resistant voltage-gated sodium channel NaV1.9 to sensory transmission and nociceptive behavior

Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR

Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor ago

Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocorti

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

Discovery of a novel class of benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain

Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist

Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists

Effects of sildenafil on erectile activity in mice lacking neuronal or endothelial nitric oxide synthase

Effects of the ventilatory stimulant, doxapram on human TASK-3 (KCNK9, K2P9.1) channels and TASK-1 (KCNK3, K2P3.1) channels

GAL-021 and GAL-160 are Efficacious in Rat Models of Obstructive and Central Sleep Apnea and Inhibit BKCa in Isolated Rat Carotid Body Glomus Cells ⬇️

Ghrelin neutralization by a ribonucleic acid-SPM ameliorates obesity in diet-induced obese mice

Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator

Identification of glucose-dependant insulin secretion targets in pancreatic beta cells by combining defined-mechanism compound library screening and siRNA gene silencing

Impaired neuropathic pain responses in mice lacking the chemokine receptor CCR2

Inhibition of soluble epoxide hydrolase attenuates endothelial dysfunction in animal models of diabetes, obesity and hypertension

Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists

Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism

Melanocortin receptors and erectile function

Pharmacokinetics and pharmacodynamics of AR9281, an inhibitor of soluble epoxide hydrolase, in single- and multiple-dose studies in healthy human subjects

Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation

Structure-activity relationship of linear tetrapeptides Tic-DPhe-Arg-Trp-NH2 at the human melanocortin-4 receptor and effects on feeding behaviors in rat.

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators

Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

The proof of the pudding is in the eating: editorial focus on "Hyperphagia, not hypometabolism, causes early onset obesity in melanocortin-4-receptor knockout mice"

The role of melanocortins in body weight regulation: opportunities for the treatment of obesity

The role of melanocortins in body weight regulation: opportunities for the treatment of obesity

The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)