2. Academic Validation
  3. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist

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

  • Science. 1991 Apr 26;252(5005):572-4. doi: 10.1126/science.1850553.
Y Yamamura 1,  H Ogawa,  T Chihara,  K Kondo,  T Onogawa,  S Nakamura,  T Mori,  M Tominaga,  Y Yabuuchi
Affiliations

Affiliation

  • 1 Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Japan.
PMID: 1850553 DOI: 10.1126/science.1850553
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.

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