Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.
Novel tricyclic benzazepine derivatives were synthesized as arginine vasopressin (AVP) antagonists. Several tricyclic compounds showed potent antagonistic activity in rat AVP receptors V(1a) and V(2). Derivatives containing pyrrolo-tricyclic amines, 13i-k, 30, and 31 also showed selectivity for the V(2) receptor.
Sum
Fuk Wah
FW
Chemical Sciences, Wyeth Research, 10965, Pearl River, NY, USA. sum@wyeth.com
Dusza
John
J
Santos
Efren Delos
ED
Grosu
George
G
Reich
Marvin
M
Du
Xumei
X
Albright
J Donald
JD
Chan
Peter
P
Coupet
Joseph
J
Ru
Xun
X
Mazandarani
Hossein
H
Saunders
Trina
T
D000818:Animals; D001127:Arginine Vasopressin / Q000037:antagonists & inhibitors*; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007202:Indicators and Reagents; D007679:Kidney Medulla / Q000187:drug effects / Q000378:metabolism; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D014563:Urodynamics / Q000187:drug effects
D001552:Benzazepines; D007202:Indicators and Reagents; D001127:Arginine Vasopressin