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Title: Vascular responses to vasopressin antagonists in man and rat.
Austin Authors: Burrell, Louise M ;Phillips, P A;Rolls, K A;Buxton, Brian F ;Johnston, Colin I;Liu, J J
Affiliation: Medicine (University of Melbourne)
Issue Date: 1-Oct-1994
Publication information: Clinical Science 1994; 87(4): 389-95
Abstract: 1. The effects of the non-peptide arginine vasopressin V1 receptor antagonist (OPC-21268) and the non-peptide V2 receptor antagonist (OPC-31260) on vasopressin-induced contraction of human internal mammary arteries and rat mesenteric resistance arteries were investigated. 2. In human internal mammary arteries, the non-peptide V1 receptor antagonist, OPC-21268, failed to antagonize vasopressin-induced contraction at low concentrations and potentiated the contraction at higher concentrations (300 nmol/l, P < 0.05). A peptide selective V1 receptor antagonist ([d(CH2)5, sarcosine7]arginine vasopressin) potently inhibited the vasopressin-induced contraction, indicating the presence of functionally constrictor V1 receptors in human internal mammary arteries. Both peptide (desGly-NH29[d(CH2)5, D-Ile2, Ile4]arginine vasopressin) and non-peptide 'selective' V2 receptor antagonists (OPC-31260, 3 mumol/l) significantly antagonized vasopressin-induced contraction (P < 0.01), indicating partial V1 receptor antagonist activity. 3. The vasopressin-induced contraction in human internal mammary arteries was reversed by high concentrations of the non-peptide V2 receptor antagonist, OPC-31260, but not by the non-peptide V1 receptor antagonist, OPC-21268. 4. The effects of OPC-21268 and OPC-31260 were specific to vascular vasopressin receptors as neither compound influenced endothelin- or noradrenaline-induced contraction in human internal mammary arteries. 5. In rat mesenteric resistance arteries, both OPC-21268 (10 nmol/l) and OPC-31260 (1 mumol/l) antagonized vasopressin-induced contraction (P < 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)
Journal: Clinical Science
Type: Journal Article
Subjects: Animals
Antidiuretic Hormone Receptor Antagonists
Arginine Vasopressin.pharmacology
Culture Techniques
Dose-Response Relationship, Drug
Mammary Arteries.drug effects.physiology
Mesenteric Artery, Superior.drug effects.physiology
Rats, Sprague-Dawley
Species Specificity
Vasoconstriction.drug effects
Appears in Collections:Journal articles

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