Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity |
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Authors: | Dyatkin Alexey B Hoekstra William J Hlasta Dennis J Andrade-Gordon Patricia de Garavilla Lawrence Demarest Keith T Gunnet Joseph W Hageman William Look Richard Maryanoff Bruce E |
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Institution: | Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, Spring House, PA 19477-0776, USA. |
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Abstract: | The synthesis and biological testing of a novel series of nonpeptide vasopressin receptor antagonists, containing a bridged bicyclic nucleus, are reported. Variation of substituents (R(1)-R(3)) in general formula 3, and the configuration of the stereocenter, resulted in potent V(2)-selective (e.g., 5) and balanced dual V(1a)/V(2) (e.g., 10) compounds. Data from receptor binding, cell-based functional, and in vivo assays are presented corrected] |
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