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Science 26 April 1991:
Vol. 252. no. 5005, pp. 572 - 574
DOI: 10.1126/science.1850553
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Articles

Science, Vol 252, Issue 5005, 572-574
Copyright © 1991 by American Association for the Advancement of Science

articles

OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist

Y Yamamura, H Ogawa, T Chihara, K Kondo, T Onogawa, S Nakamura, T Mori, M Tominaga, and Y Yabuuchi

Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Japan.

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.


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