Abstract
8-Aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes represent a novel series of high-affinity corticotropin-releasing factor-1 receptor (CRF1R) antagonists. Herein we report the synthesis and SAR around the tricyclic core and the anxiolytic activity of an orally dosed exemplary compound 9d (K(i)=8.0 nM) in a mouse canopy model.
MeSH terms
-
Administration, Oral
-
Animals
-
Antidepressive Agents / pharmacology
-
Aza Compounds / chemistry
-
Depression / drug therapy
-
Dose-Response Relationship, Drug
-
Indenes / chemistry
-
Kinetics
-
Mice
-
Mice, Inbred BALB C
-
Models, Chemical
-
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
-
Solubility
-
Structure-Activity Relationship
-
Time Factors
-
Water / chemistry
Substances
-
Antidepressive Agents
-
Aza Compounds
-
Indenes
-
Receptors, Corticotropin-Releasing Hormone
-
Water