Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.
Bioorg Med Chem Lett
; 15(6): 1565-71, 2005 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-15745798
ABSTRACT
We have identified and synthesized a series of phenyl-tetrazolyl and 4-thiopyridyl indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation, as well as PK properties, led to the discovery of 28 (EC50=186 nM), which displayed activity in a rodent model for schizophrenia.
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Base de dados:
MEDLINE
Assunto principal:
Receptores de Glutamato Metabotrópico
/
Indanos
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article