Pyrazinobenzodiazepines as Potent Nonpeptide Vasopressin Receptor Antagonists

Author(s): Jay M. Matthews, Dennis J. Hlasta, Patricia Andrade-Gordon, Keith T. Demarest, Eric Ericson, Joseph W. Gunnet, William Hageman, Richard Look, John B. Moore, Bruce E. Maryanoff.

Journal Name: Letters in Drug Design & Discovery

Volume 2 , Issue 3 , 2005

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We have identified a novel series of tricyclic pyrazinobenzodiazepines, represented by general structure 2, as potent vasopressin receptor antagonists. For example, 3 binds with high affinity to human V2 receptors and is very selective relative to V1a receptors. Compound (R)-(+)-3 exhibited pronounced aquaretic activity in rats and dogs on oral administration.

Keywords: g-protein-coupled receptors, smooth muscle contraction, glycogen, corticotropin, oxazinobenzodiazepines, hydrophobicity, secondary amine, crystallization, oxygen systems

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Article Details

Year: 2005
Page: [219 - 223]
Pages: 5
DOI: 10.2174/1570180053765183
Price: $65

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