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ID: ALA1146755
Journal: Bioorg Med Chem Lett
Title: Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.
Authors: Matthews JM, Hoekstra WJ, Dyatkin AB, Hecker LR, Hlasta DJ, Poulter BL, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Reynolds CH, Maryanoff BE.
Abstract: Vasopressin receptor antagonists can elicit ion-sparing diuretic effects (i.e., aquaresis) in vivo by blunting the action of the circulating hypophyseal hormone arginine vasopressin. We have identified two new series of basic tricyclic benzodiazepines, represented by general structure 1, which contain compounds that bind with high affinity to human V2 receptors. For example, (S)-(+)-8 and 5 are potent and selective V2 receptor antagonists with pronounced aquaretic activity in rats on oral administration.
CiteXplore: 15125926