Author/Authors :
Jay M. Matthews، نويسنده , , Michael N. Greco، نويسنده , , Leonard R. Hecker، نويسنده , , William J. Hoekstra، نويسنده , , Patricia Andrade-Gordon، نويسنده , , Lawrence de Garavilla، نويسنده , , Keith T. Demarest، نويسنده , , Eric Ericson، نويسنده , , Joseph W. Gunnet، نويسنده , , William Hageman، نويسنده , , Richard Look، نويسنده , , John B. Moore، نويسنده , , Bruce E. Maryanoff، نويسنده ,
Abstract :
A series of novel 3,4,5,6-tetrahydro-1H-azepino[4,3,2-cd]indoles was synthesized and tested for vasopressin receptor antagonist activity. We identified compounds with high affinity for the human V2 receptor and good selectivity over the human V1a receptor. Compound 6c bound to V2 receptors with an IC50 value of 20 nM, had >100-fold selectivity over V1a receptors, and inhibited cAMP formation in a cellular V2 functional assay with an IC50 value of 70 nM.
