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

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.
AuthorsY Yamamura, H Ogawa, T Chihara, K Kondo, T Onogawa, S Nakamura, T Mori, M Tominaga, Y Yabuuchi
JournalScience (New York, N.Y.) (Science) Vol. 252 Issue 5005 Pg. 572-4 (Apr 26 1991) ISSN: 0036-8075 [Print] United States
PMID1850553 (Publication Type: Journal Article)
Chemical References
  • Piperidines
  • Quinolones
  • Receptors, Angiotensin
  • Receptors, Vasopressin
  • Angiotensin II
  • Arginine Vasopressin
  • OPC 21268
  • Norepinephrine
Topics
  • Administration, Oral
  • Angiotensin II (pharmacology)
  • Animals
  • Arginine Vasopressin (antagonists & inhibitors, metabolism, pharmacology)
  • Binding, Competitive
  • Blood Pressure (drug effects)
  • Cell Membrane (metabolism)
  • Kidney (metabolism)
  • Kinetics
  • Liver (metabolism)
  • Norepinephrine (pharmacology)
  • Piperidines (administration & dosage, pharmacology)
  • Quinolones (administration & dosage, pharmacology)
  • Rats
  • Receptors, Angiotensin (drug effects, metabolism)
  • Receptors, Vasopressin
  • Time Factors

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