| Pharmacology of bucindolol in isolated canine vascular smooth muscle. | |
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MedLine Citation:
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PMID: 6149305 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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To determine the effects of bucindolol on isolated vascular smooth muscle, rings of canine coronary and femoral arteries and saphenous veins were suspended for isometric tension recording in organ chambers filled with physiological salt solution. Bucindolol (3 X 10(-10) to 1 X 10(-7) M) had a comparable inhibitory effect on relaxations induced by isoproterenol in coronary arteries (which contain postjunctional beta-1 adrenoceptors) and saphenous veins (which contain postjunctional beta-2 adrenoceptors). Bucindolol (1 X 10(-7) M) had no effect on relaxations induced by sodium nitroprusside during contractions evoked by prostaglandin F2 alpha in either saphenous veins or coronary arteries. Bucindolol also had weak (relative to its beta adrenoceptor effect) alpha adrenoceptor-antagonistic activity that was greater for postjunctional alpha-1 than alpha-2 adrenoceptors. In all tissues tested, bucindolol in concentrations greater than 1 X 10(-6) M caused relaxations of responses induced by various nonadrenergic agonists. Propranolol (5 X 10(-6) M) did not alter the direct inhibitory effect that bucindolol had on contractions of coronary arteries or saphenous veins evoked by prostaglandin F2 alpha; this inhibitory effect of bucindolol was independent of the endothelium. In superfused saphenous vein strips, previously incubated with [3H]norepinephrine, bucindolol (3 X 10(-7) to 1 X 10(-5) M) increased the basal efflux of [3H]norepinephrine and its [3H] metabolites. Bucindolol at 1 X 10(-7) M inhibited prejunctional beta adrenoceptors without affecting prejunctional alpha adrenoceptors. These experiments indicate that bucindolol in decreasing orders of activity 1) has nonselective beta adrenoceptor-antagonistic properties, 2) has a selective alpha-1 adrenoceptor-inhibitory effect and 3) has a nonspecific direct relaxing action on vascular smooth muscle. |
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Authors:
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T J Rimele; L L Aarhus; R R Lorenz; T W Rooke; P M Vanhoutte |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: The Journal of pharmacology and experimental therapeutics Volume: 231 ISSN: 0022-3565 ISO Abbreviation: J. Pharmacol. Exp. Ther. Publication Date: 1984 Nov |
Date Detail:
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Created Date: 1984-12-19 Completed Date: 1984-12-19 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0376362 Medline TA: J Pharmacol Exp Ther Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 317-25 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adrenergic beta-Antagonists
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pharmacology* Animals Azepines / pharmacology Dogs Dose-Response Relationship, Drug Electric Stimulation Female Isoproterenol / pharmacology Male Muscle, Smooth, Vascular / drug effects* Norepinephrine / pharmacology Propanolamines / pharmacology* Receptors, Adrenergic, alpha / drug effects Receptors, Adrenergic, beta / drug effects |
| Grant Support | |
ID/Acronym/Agency:
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HL05883/HL/NHLBI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Adrenergic beta-Antagonists; 0/Azepines; 0/Propanolamines; 0/Receptors, Adrenergic, alpha; 0/Receptors, Adrenergic, beta; 36085-73-1/talipexole; 51-41-2/Norepinephrine; 70369-47-0/bucindolol; 7683-59-2/Isoproterenol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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