Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.
ACS Med Chem Lett
; 1(8): 406-10, 2010 Nov 11.
Article
en En
| MEDLINE
| ID: mdl-24900224
Novel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physical and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads. Compound 20 (TBPCOB) was shown to have robust activity in a PCP-induced hyperlocomotion model in rat, an assay responsive to clinical antipsychotic treatments for schizophrenia.
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Colección:
01-internacional
Base de datos:
MEDLINE
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En
Revista:
ACS Med Chem Lett
Año:
2010
Tipo del documento:
Article
Pais de publicación:
Estados Unidos