vestipitant and Depressive-Disorder

vestipitant has been researched along with Depressive-Disorder* in 1 studies

Other Studies

1 other study(ies) available for vestipitant and Depressive-Disorder

Article	Year
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clini Journal of medicinal chemistry, 2011, Feb-24, Volume: 54, Issue:4 A large body of compelling preclinical evidence supports the clinical use of neurokinin (NK) receptor antagonists in a plethora of CNS and non-CNS therapeutic areas. The significant investment made in this area over the past 2 decades culminated with the observation that NK(1) receptor antagonists elicited clinical efficacy in major depression disorders. In addition, aprepitant (Merck) was launched as a new drug able to prevent chemotherapy-induced nausea and vomiting (CINV). After the discovery by GlaxoSmithKline of vestipitant, a wide drug discovery program was launched aimed at identifying additional clinical candidates. New compounds were designed to maximize affinity at the NK(1) receptor binding site while retaining suitable physicochemical characteristics to ensure excellent pharmacokinetic and pharmacodynamic properties in vivo. Herein we describe the discovery process of a new NK(1) receptor antagonist (casopitant) selected as clinical candidate and progressed into clinical studies to treat major depression disorders. Topics: Animals; Behavior, Animal; Brain; CHO Cells; Cricetinae; Cricetulus; Depressive Disorder; Drug Discovery; Gerbillinae; Half-Life; Humans; Magnetic Resonance Spectroscopy; Neurokinin-1 Receptor Antagonists; Piperazines; Piperidines; Regression Analysis; Spectrometry, Mass, Electrospray Ionization; Spectrophotometry, Infrared; Stereoisomerism	2011

Article

Year

Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clini

Journal of medicinal chemistry, 2011, Feb-24, Volume: 54, Issue:4

A large body of compelling preclinical evidence supports the clinical use of neurokinin (NK) receptor antagonists in a plethora of CNS and non-CNS therapeutic areas. The significant investment made in this area over the past 2 decades culminated with the observation that NK(1) receptor antagonists elicited clinical efficacy in major depression disorders. In addition, aprepitant (Merck) was launched as a new drug able to prevent chemotherapy-induced nausea and vomiting (CINV). After the discovery by GlaxoSmithKline of vestipitant, a wide drug discovery program was launched aimed at identifying additional clinical candidates. New compounds were designed to maximize affinity at the NK(1) receptor binding site while retaining suitable physicochemical characteristics to ensure excellent pharmacokinetic and pharmacodynamic properties in vivo. Herein we describe the discovery process of a new NK(1) receptor antagonist (casopitant) selected as clinical candidate and progressed into clinical studies to treat major depression disorders.

Topics: Animals; Behavior, Animal; Brain; CHO Cells; Cricetinae; Cricetulus; Depressive Disorder; Drug Discovery; Gerbillinae; Half-Life; Humans; Magnetic Resonance Spectroscopy; Neurokinin-1 Receptor Antagonists; Piperazines; Piperidines; Regression Analysis; Spectrometry, Mass, Electrospray Ionization; Spectrophotometry, Infrared; Stereoisomerism

2011