| SK&F 87516, a close analog of fenoldopam, is a partial agonist at dopamine-1 and alpha-2 receptors and produces stimulation of 5-hydroxytryptamine-2 receptors in the cardiovascular system of the rat. | |
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MedLine Citation:
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PMID: 1672375 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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In pentobarbital-anesthetized rats, SK&F 87516 (1.25-80 micrograms/kg/min intravenously over 15 min), the fluoro analog of the selective DA-1 dopamine receptor agonist fenoldopam produced dose-related decreases in carotid artery blood pressure that faded during the infusion period. These effects were abolished by SCH 23390, prolonged by ritanserin, but unchanged by bilateral vagotomy, atenolol, ICI 118,551, idazoxan, methylatropine or S-sulpiride. SK&F 87516 also inhibited the hypotensive effects of clonidine and of the DA-1 receptor agonist fenoldopam, but not of acetylcholine. In pithed rats, SK&F 87516 produced a biphasic vasopressor response. The initial phase was enhanced by SCH 23390 and converted to a transient hypotension by idazoxan. The secondary response was inhibited by ritanserin and enalapril. In pithed, but not in intact rats, SK&F 87516 increased plasma renin activity. In intact rats, SK&F 87516 produced dose-related bradycardic effects that were inhibited (50%) by idazoxan, methylatropine or bilateral vagotomy and abolished by chlorisondamine or pithing. In pithed rats pretreated with either saline or idazoxan, SK&F 87516 reduced the tachycardia to electrical stimulation of preganglionic more than that to postganglionic cardioaccelerator nerve fibers. However, it did not modify heart rate increases evoked by intravenous norepinephrine. In conclusion, SK&F 87516 produces hypotension via vascular DA-1 receptor stimulation. The fading of this effect during the infusion of SK&F 87516 may be related to the partial agonist property of this compound at DA-1 receptors and the stimulation of 5-hydroxytryptamine-2 receptors. SK&F 87516 also behaves as a partial agonist at alpha-2 adrenoceptors.(ABSTRACT TRUNCATED AT 250 WORDS) |
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Authors:
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A C Le Monnier de Gouville; K Lawson; C Thiry; I Cavero |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: The Journal of pharmacology and experimental therapeutics Volume: 256 ISSN: 0022-3565 ISO Abbreviation: J. Pharmacol. Exp. Ther. Publication Date: 1991 Mar |
Date Detail:
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Created Date: 1991-04-24 Completed Date: 1991-04-24 Revised Date: 2007-11-15 |
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: 1049-56 Citation Subset: IM |
Affiliation:
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Centre de Recherche de Vitry-Alfortville, Vitry sur Seine, France. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
/
administration & dosage,
analogs & derivatives*,
pharmacokinetics,
pharmacology Animals Cardiovascular System / drug effects* Dopamine Agents / administration & dosage, pharmacokinetics, pharmacology* Fenoldopam Hemodynamics / drug effects Infusions, Intravenous Injections, Intravenous Male Norepinephrine / blood Rats Receptors, Dopamine / drug effects* Receptors, Serotonin / drug effects* Renin / blood Vasodilator Agents / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Dopamine Agents; 0/Receptors, Dopamine; 0/Receptors, Serotonin; 0/Vasodilator Agents; 51-41-2/Norepinephrine; 67227-56-9/Fenoldopam; 67287-49-4/2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; 72912-26-6/SK&F R87516; EC 3.4.23.15/Renin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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