| Integrative cardiovascular actions of a novel catecholamine, GP-2-128. | |
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MedLine Citation:
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PMID: 7515995 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Systematic modification in the chemical structure of dobutamine resulted in production of a long-acting, highly potent catecholamine, GP-2-128 [(1-(3,4-dihydroxyphenyl)-2-[3-(4-carbamyl phenyl)-1-methylpropylamino] ethanol)]. The cardiovascular actions of GP-2-128 were compared with those of isoproterenol (ISO) and dobutamine (DOB) in anesthetized dogs. GP-2-128 significantly increased left ventricular pressure (LVdP/dtmax), cardiac output (CO), and heart rate (HR). It also reduced total peripheral vascular resistance (TPVR). For a given increase in contractility, changes in HR were greater after ISO than after GP-2-128 administration. DOB did not change HR significantly. Both GP-2-128 and DOB reduced TPVR, but ISO was more effective than GP-2-128 and DOB in reducing TPVR. GP-2-128 was 18,000 and 52 times more potent than DOB and ISO, respectively, in increasing LVdP/dtmax. For a given increase in contractility, the cardiovascular actions of GP-2-128 lasted significantly longer than those of DOB or ISO. A 50% mixture of the RR and RS distereoisomer forms of GP-2-128 (GP-2-114) have the same pharmacologic profile as the pure RR distereoisomer. Both GP-2-128 and GP-2-114 produced current-dependent cardiovascular actions when administered by transdermal iontophoresis. The inotropic and chronotropic effects of GP-2-128 are both largely due to stimulation of beta-adrenoceptors, as shown by receptor blockade with propranolol. GP-2-128 is a very potent, long-acting catecholamine that can be administered by other than intravenous (i.v.) route. |
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Authors:
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G Abou-Mohamed; R W Caldwell; T M Ibrahim; R R Tuttle |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Journal of cardiovascular pharmacology Volume: 23 ISSN: 0160-2446 ISO Abbreviation: J. Cardiovasc. Pharmacol. Publication Date: 1994 Mar |
Date Detail:
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Created Date: 1994-07-11 Completed Date: 1994-07-11 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 7902492 Medline TA: J Cardiovasc Pharmacol Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 485-91 Citation Subset: IM |
Affiliation:
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Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta 30912. |
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 Benzamides / administration & dosage, pharmacology* Cardiac Output / drug effects Cardiovascular Agents / administration & dosage, pharmacology* Catecholamines / administration & dosage, pharmacology* Dobutamine / pharmacology Dogs Female Half-Life Heart Rate / drug effects Hemodynamics / drug effects* Injections, Intravenous Iontophoresis Isoproterenol / pharmacology Male Muscle Contraction / drug effects Myocardial Contraction / drug effects Stereoisomerism Vascular Resistance / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Adrenergic beta-Antagonists; 0/Benzamides; 0/Cardiovascular Agents; 0/Catecholamines; 130783-39-0/1-(3,4-dihydroxyphenyl)-2-(3-(4-carbamylphenyl)-1-methylpropylamino)ethanol; 34368-04-2/Dobutamine; 7683-59-2/Isoproterenol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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