Novel, potent, selective and brain penetrant vasopressin 1b receptor antagonists
2018
Abstract Herein we report the discovery of a novel
oxindole-based series of vasopressin 1b (V1b)
receptor antagonists. Introducing a substituted
piperazinemoiety and optimizing the southern and the northern aromatic rings resulted in potent, selective and brain penetrant V1b
receptor antagonists. Compound 9c was found to be efficacious in a rat model of anti-depressant activity (3 mg/kg, ip). Interestingly, both moderate terminal half-life and moderate bioavailability could be achieved despite sub-optimal microsomal stability.
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