Title of article
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
753
To page
756
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793009
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