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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||URI:||http://ahro.austin.org.au/austinjspui/handle/1/13406||URL:||https://pubmed.ncbi.nlm.nih.gov/8549062||Type:||Journal Article||Subjects:||Antidiuretic Hormone Receptor Antagonists
Arginine Vasopressin.antagonists & inhibitors
Muscle Contraction.drug effects
|Appears in Collections:||Journal articles|
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