title: Orally active, nonpeptide vasopressin V2 receptor antagonists: a novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds.
abstract: This paper describes a novel series of nonpeptide vasopressin V2 receptor antagonists. It has been demonstrated that the 1-[4-(benzoylamino)benzoyl]-2,3,4,5-1H-benzazepines and 1-[4-(benzoylamino)benzoyl]-2,3,4,5-1H-1,5-benzodiazepines show a high affinity for V2 (and V1a) receptors. Among the 1-[4-(benzoylamino)benzoyl]-2,3,4,5-1H-benzazepine series, compounds with an alkylamino group on the benzazepine ring have been shown to have oral activity. A lipophilic group at the ortho position on the terminal benzoyl ring is important for both high V2 receptor affinity and oral activity. On the basis of these favorable properties, clinical testing of 31b has begun for use as an oral and iv aquaretic agent.
authors.affiliation: Second Institute of New Drug Research, Otsuka Pharmaceutical Co., Tokushima, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Ogawa
authors.forename: H
authors.initials: H
authors.lastname: Yamashita
authors.forename: K
authors.initials: K
authors.lastname: Kondo
authors.forename: Y
authors.initials: Y
authors.lastname: Yamamura
authors.forename: H
authors.initials: H
authors.lastname: Miyamoto
authors.forename: K
authors.initials: K
authors.lastname: Kan
authors.forename: K
authors.initials: K
authors.lastname: Kitano
authors.forename: M
authors.initials: M
authors.lastname: Tanaka
authors.forename: K
authors.initials: K
authors.lastname: Nakaya
authors.forename: S
authors.initials: S
authors.lastname: Nakamura
authors.forename: T
authors.initials: T
authors.lastname: Mori
authors.forename: M
authors.initials: M
authors.lastname: Tominaga
authors.forename: Y
authors.initials: Y
authors.lastname: Yabuuchi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines