Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Bioorg Med Chem Lett
; 17(5): 1386-91, 2007 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-17210250
ABSTRACT
This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to a unique allosteric binding site distinct from other mGluR5 PAMs, CPPHA has been the focus of numerous pharmacology studies by several laboratories.
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Base de dados:
MEDLINE
Assunto principal:
Ftalimidas
/
Benzamidas
/
Receptores de Glutamato Metabotrópico
/
Regulação Alostérica
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article