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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. doi: 10.1016/j.bmcl.2009.09.050. Epub 2009 Sep 17.

Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.

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Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.


Vasopressin 1b (V1b) antagonists have been postulated as possible treatments for depression and anxiety. A novel series of potent and selective V1b antagonists has been identified starting from an in-house screen hit. The incorporation of a sulfonamide linker between a tetrahydroisoquinoline core and amino piperidine lead to the identification of a V1b antagonist with similar affinity for human and rat receptors. Further optimization of the right hand portion afforded potent V1b antagonists that possessed moderate to high selectivity over other receptors.

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