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)...

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Bibliographic Details
Published in:Science (American Association for the Advancement of Science) 1991-04, Vol.252 (5005), p.572-574
Main Authors: Yamamura, Yoshitaka, Ogawa, Hidenori, Chihara, Tomihiko, Kondo, Kazumi, Onogawa, Toshiyuki, Nakamura, Shigeki, Mori, Toyoki, Tominaga, Michiaki, Yabuuchi, Youichi
Format: Article
Language:English
Subjects:
Administration, Oral
Angiotensin II - pharmacology
Animals
Antibodies
Arginine Vasopressin - antagonists & inhibitors
Arginine Vasopressin - metabolism
Arginine Vasopressin - pharmacology
Binding, Competitive
Biochemistry
Biological and medical sciences
Blood pressure
Blood Pressure - drug effects
Cell Membrane - metabolism
Cell membranes
Dosage
Dose response relationship
Drugs
Heart
Hormones. Endocrine system
Kidney - metabolism
Kidneys
Kinetics
Liver
Liver - metabolism
Medical sciences
Norepinephrine - pharmacology
P branes
Pharmacology. Drug treatments
Piperidines - administration & dosage
Piperidines - pharmacology
Quinolones - administration & dosage
Quinolones - pharmacology
Rats
Receptors
Receptors, Angiotensin - drug effects
Receptors, Angiotensin - metabolism
Receptors, Vasopressin
Spectral bands
Therapy
Time Factors
Vasoconstrictor agents
Vasoconstrictors
Vasopressin
Vasopressins
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Summary: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.
ISSN:0036-8075
1095-9203
DOI:10.1126/science.1850553