title: Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.
abstract: 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.
authors.affiliation: Chemical Sciences, Wyeth Research, 10965, Pearl River, NY, USA. sum@wyeth.com
authors.forename: Fuk Wah
authors.initials: FW
authors.lastname: Sum
authors.forename: John
authors.initials: J
authors.lastname: Dusza
authors.forename: Efren Delos
authors.initials: ED
authors.lastname: Santos
authors.forename: George
authors.initials: G
authors.lastname: Grosu
authors.forename: Marvin
authors.initials: M
authors.lastname: Reich
authors.forename: Xumei
authors.initials: X
authors.lastname: Du
authors.forename: J Donald
authors.initials: JD
authors.lastname: Albright
authors.forename: Peter
authors.initials: P
authors.lastname: Chan
authors.forename: Joseph
authors.initials: J
authors.lastname: Coupet
authors.forename: Xun
authors.initials: X
authors.lastname: Ru
authors.forename: Hossein
authors.initials: H
authors.lastname: Mazandarani
authors.forename: Trina
authors.initials: T
authors.lastname: Saunders
mesh_terms: 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
chemical_list: D001552:Benzazepines; D007202:Indicators and Reagents; D001127:Arginine Vasopressin