OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist.
An orally effective, nonpeptide, vasopressin V1 receptor antagonist, OPC-21268, has been identified. This compound selectively antagonized binding to the V1 subtype of the vasopressin receptor in a competitive manner. In vivo, the compound acted as a specific antagonist of arginine vasopressin (AVP)-induced vasoconstriction. After oral administration in conscious rats, the compound also antagonized pressor responses to AVP. OPC-21268 can be used to study the physiological role of AVP and may be therapeutically useful in the treatment of hypertension and congestive heart failure.
Yamamura
Y
Y
Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Japan.
Ogawa
H
H
Chihara
T
T
Kondo
K
K
Onogawa
T
T
Nakamura
S
S
Mori
T
T
Tominaga
M
M
Yabuuchi
Y
Y
D000284:Administration, Oral; D000804:Angiotensin II / Q000494:pharmacology; D000818:Animals; D001127:Arginine Vasopressin / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology*; D001667:Binding, Competitive; D001794:Blood Pressure / Q000187:drug effects*; D002462:Cell Membrane / Q000378:metabolism; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D009638:Norepinephrine / Q000494:pharmacology; D010880:Piperidines / Q000008:administration & dosage / Q000494:pharmacology*; D015363:Quinolones / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D011945:Receptors, Angiotensin / Q000187:drug effects* / Q000378:metabolism; D017483:Receptors, Vasopressin; D013997:Time Factors
D010880:Piperidines; D015363:Quinolones; D011945:Receptors, Angiotensin; D017483:Receptors, Vasopressin; D000804:Angiotensin II; D001127:Arginine Vasopressin; C068644:OPC 21268; D009638:Norepinephrine