1.
Bioorg Med Chem Lett
; 14(11): 2747-52, 2004 Jun 07.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15125926
RESUMO
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.