title: Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.
abstract: A novel series of spirobenzazepines was synthesized and evaluated for V1a and V2 receptor antagonist activity. Compounds 8b, 8i, and 8k have shown selective V1a receptor antagonist activity. Compounds 8p and 8q were shown to be dual V1a/V2 receptor antagonists.
authors.affiliation: Endocrine Therapeutics and Metabolic Disorders, Johnson and Johnson Pharmaceutical Research and Development, L.L.C. 1000 Route 202, Bldg: PCC; Room: PC110, Raritan, NJ 08869-0602, USA.
authors.forename: Min Amy
authors.initials: MA
authors.lastname: Xiang
authors.forename: Robert H
authors.initials: RH
authors.lastname: Chen
authors.forename: Keith T
authors.initials: KT
authors.lastname: Demarest
authors.forename: Joseph
authors.initials: J
authors.lastname: Gunnet
authors.forename: Richard
authors.initials: R
authors.lastname: Look
authors.forename: William
authors.initials: W
authors.lastname: Hageman
authors.forename: William V
authors.initials: WV
authors.lastname: Murray
authors.forename: Donald W
authors.initials: DW
authors.lastname: Combs
authors.forename: Mona
authors.initials: M
authors.lastname: Patel
mesh_terms: D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D000242:Cyclic AMP / Q000032:analysis; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D011485:Protein Binding; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines; D008024:Ligands; D013141:Spiro Compounds; D000242:Cyclic AMP