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Title: Potent inhibitory effect of SR 49059, an orally active non-peptide vasopressin VIa receptor antagonist, on human arterial coronary bypass graft.
Austin Authors: Liu, J J;Chen, J R;Buxton, Brian F ;Johnston, Colin I;Burrell, Louise M 
Affiliation: Department of Cardiac Surgery, University of Melbourne, Austin, Australia
Issue Date: 1-Nov-1995
Publication information: Clinical Science 1995; 89(5): 481-5
Abstract: 1. The effect of vasopressin receptor antagonists varies between analogues (peptide, non-peptide) and across species. In this study the effect of the novel non-peptide vasopressin V1a receptor antagonist SR 49059 on human internal mammary arteries was investigated. 2. SR 49059 produced a potent, concentration-dependent, inhibitory effect on vasopressin-induced contraction of human coronary bypass graft internal mammary arteries. Both SR 49059 (1 mumol/l) and a peptide selective V1a antagonist ([d(CH2)5sarcosine7]arginine vasopressin) (1 mumol/l) abolished vasopressin-induced contraction. The non-peptide V1a receptor antagonist OPC-21268 (1 mumol/l) had no effect on vasopressin-induced contraction. 3. The effect of SR 49059 was specific to vascular vasopressin receptors as noradrenaline-induced contraction was not influenced by SR 49059. 4. The results of this study in vitro indicate that the non-peptide SR 49059 is a potent, specific vasopressin V1a receptor antagonist in the human internal mammary artery and suggest that it may be a useful tool for studying the pathophysiological role of vasopressin in man.
Gov't Doc #: 8549062
Type: Journal Article
Subjects: Antidiuretic Hormone Receptor Antagonists
Arginine Vasopressin.antagonists & inhibitors
Arteries.drug effects
Hormone Antagonists.pharmacology
Mammary Arteries
Muscle Contraction.drug effects
Appears in Collections:Journal articles

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