Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.

Di Fabio, Romano; Griffante, Cristiana; Alvaro, Giuseppe; Pentassuglia, Giorgio; Pizzi, Domenica A; Donati, Daniele; Rossi, Tino; Guercio, Giuseppe; Mattioli, Mario; Cimarosti, Zadeo; Marchioro, Carla; Provera, Stefano; Zonzini, Laura; Montanari, Dino; Melotto, Sergio; Gerrard, Philip A; Trist, David G; Ratti, Emiliangelo; Corsi, Mauro

Di Fabio, Romano; Griffante, Cristiana; Alvaro, Giuseppe; Pentassuglia, Giorgio; Pizzi, Domenica A; Donati, Daniele; Rossi, Tino; Guercio, Giuseppe; Mattioli, Mario; Cimarosti, Zadeo; Marchioro, Carla; Provera, Stefano; Zonzini, Laura; Montanari, Dino; Melotto, Sergio; Gerrard, Philip A; Trist, David G; Ratti, Emiliangelo; Corsi, Mauro.

Di Fabio R; Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline Medicines Research Centre, Via A. Fleming 4, 37135 Verona, Italy. rdf26781@gsk.com

J Med Chem ; 52(10): 3238-47, 2009 May 28.

Article en En | MEDLINE | ID: mdl-19388677

Asunto(s)

Antagonistas del Receptor de Neuroquinina-1; Piperazinas/química; Piperidinas/farmacología; Administración Oral; Animales; Células CHO; Cricetinae; Cricetulus; Descubrimiento de Drogas; Evaluación Preclínica de Medicamentos; Fluorobencenos; Gerbillinae; Farmacocinética; Piperazinas/farmacología; Piperidinas/farmacocinética; Relación Estructura-Actividad

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piperazinas / Piperidinas / Antagonistas del Receptor de Neuroquinina-1 Límite: Animals Idioma: En Año: 2009 Tipo del documento: Article

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