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OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist
Y Yamamura1, H Ogawa, T Chihara
1Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Japan.
Science (New York, N.Y.)
|April 26, 1991
Abstract:
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.