7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.
We previously reported a series of benzazepine derivatives as orally active nonpeptide arginine vasopressin (AVP) V2 receptor antagonists. After the lead structure OPC-31260 was structurally evaluated and optimized, the introduction of the 7-Cl moiety on the benzazepine and 2-CH3 on the aminobenzoyl moiety enhanced its oral activity. The new AVP-V2 selective antagonist OPC-41061 was determined to be a potent and orally active agent.
Kondo
K
K
Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd., Japan.
Ogawa
H
H
Yamashita
H
H
Miyamoto
H
H
Tanaka
M
M
Nakaya
K
K
Kitano
K
K
Yamamura
Y
Y
Nakamura
S
S
Onogawa
T
T
Mori
T
T
Tominaga
M
M
D000818:Animals; D065092:Antidiuretic Hormone Receptor Antagonists; D001127:Arginine Vasopressin / Q000378:metabolism; D001552:Benzazepines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004232:Diuretics / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D015394:Molecular Structure; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D017483:Receptors, Vasopressin / Q000378:metabolism; D000077602:Tolvaptan
D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines; D004232:Diuretics; D017483:Receptors, Vasopressin; D001127:Arginine Vasopressin; D000077602:Tolvaptan