Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.
Bioorg Med Chem Lett
; 21(23): 6955-9, 2011 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-22030026
ABSTRACT
Herein we report the discovery and SAR of a novel antagonist of metabotropic glutamate receptor 4 (mGlu(4)). The antagonist was discovered via a molecular switch from a closely related mGlu(4) positive allosteric modulator (PAM). This antagonist (VU0448383) displays an IC(50) value of 8.2±0.4 µM and inhibits an EC(80) glutamate response by 63.1±6.6%.
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Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Desenho de Fármacos
/
Receptores de Glutamato Metabotrópico
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article