Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).
J Med Chem
; 62(3): 1690-1695, 2019 02 14.
Article
em En
| MEDLINE
| ID: mdl-30608678
ABSTRACT
Herein, we report the discovery of a new, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu7) negative allosteric modulator (NAM) that achieves exposure in cerebral spinal fluid (CSF) 2.5× above the in vitro IC50 at minimum effective doses (MEDs) of 3 mg/kg in preclinical anxiety models.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Ansiolíticos
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Triazóis
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Benzamidas
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Encéfalo
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Receptores de Glutamato Metabotrópico
Limite:
Animals
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article