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The known interactions between the serotonergic and neurokinin systems suggest that serotonin reuptake inhibitor (SSRIs) efficacy may be improved by neurokinin-1 receptor (NK1R) antagonism. In the current studies combination of a subeffective dose of an SSRI (0.3 mg/kg fluoxetine or 0.03 mg/kg citalopram) with a subeffective dose of an NK1R antagonist (0.3 mg/kg aprepitant or 1 mg/kg CP-122,721) produced...
BMS-763534 is a potent (CRF 1 IC 50 = 0.4 nM) and selective (>1000-fold selectivity vs. all other sites tested) CRF 1 receptor antagonist (pA2 = 9.47 vs. CRF 1 -mediated cAMP production in Y79 cells). BMS-763534 accelerated the dissociation of 125 I-o-CRF from rat frontal cortex membrane CRF 1 receptors consistent with a negative allosteric modulation...
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