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.
MeSH terms
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Administration, Oral
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Angiotensin II / pharmacology
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Animals
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Arginine Vasopressin / antagonists & inhibitors
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Arginine Vasopressin / metabolism
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Arginine Vasopressin / pharmacology*
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Binding, Competitive
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Blood Pressure / drug effects*
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Cell Membrane / metabolism
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Kidney / metabolism
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Kinetics
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Liver / metabolism
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Norepinephrine / pharmacology
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Piperidines / administration & dosage
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Piperidines / pharmacology*
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Quinolones / administration & dosage
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Quinolones / pharmacology*
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Rats
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Receptors, Angiotensin / drug effects*
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Receptors, Angiotensin / metabolism
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Receptors, Vasopressin
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Time Factors
Substances
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Piperidines
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Quinolones
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Receptors, Angiotensin
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Receptors, Vasopressin
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Angiotensin II
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Arginine Vasopressin
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OPC 21268
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Norepinephrine