Pharmacological and behavioral characterization of the novel CRF1 antagonist BMS-763534

► BMS-763534, a potent and selective novel CRF1 receptor antagonist, is characterized. ► BMS-763534 acted as a negative allosteric modulator of CRF binding. ► BMS-763534 was anxiolytic at doses producing ≥70% CRF1 receptor occupancy in the brain. ► A BMS-763534 metabolite was a low potency potentiator of GABA currents.