Your browser doesn't support javascript.
loading
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Sheffler, Douglas J; Wenthur, Cody J; Bruner, Joshua A; Carrington, Sheridan J S; Vinson, Paige N; Gogi, Kiran K; Blobaum, Anna L; Morrison, Ryan D; Vamos, Mitchell; Cosford, Nicholas D P; Stauffer, Shaun R; Daniels, J Scott; Niswender, Colleen M; Conn, P Jeffrey; Lindsley, Craig W.
Afiliação
  • Sheffler DJ; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Bioorg Med Chem Lett ; 22(12): 3921-5, 2012 Jun 15.
Article em En | MEDLINE | ID: mdl-22607673
ABSTRACT
Herein we report the discovery and SAR of a novel metabotropic glutamate receptor 3 (mGlu(3)) NAM probe (ML289) with 15-fold selectivity versus mGlu(2). The mGlu(3) NAM was discovered via a 'molecular switch' from a closely related, potent mGlu(5) positive allosteric modulator (PAM), VU0092273. This NAM (VU0463597, ML289) displays an IC(50) value of 0.66 µM and is inactive against mGlu(5).
Assuntos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidinas / Microssomos Hepáticos / Sondas Moleculares / Receptores de Glutamato Metabotrópico Tipo de estudo: Diagnostic_studies Limite: Humans Idioma: En Ano de publicação: 2012 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidinas / Microssomos Hepáticos / Sondas Moleculares / Receptores de Glutamato Metabotrópico Tipo de estudo: Diagnostic_studies Limite: Humans Idioma: En Ano de publicação: 2012 Tipo de documento: Article