| Pharmacological properties of 5-[(6,7,8-trimethoxy-4-quinazolinyl) amino]-1-pentanyl nitrate maleate in cardiovascular system. | |
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MedLine Citation:
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PMID: 1815519 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Effects of 5-[6,7,8-trimethoxy-4-quinazolinyl)amino]-1-pentanyl nitrate maleate (KT-1, CAS 47487-05-8), whose chemical structure has both a prazosin and a nitrate moiety, on cardiovascular system were investigated in in vivo and in vitro experiments. KT-1 i.v. decreased aortic pressure, renal blood flow, left ventricular enddiastolic pressure and resistances of total peripheral, vertebral, coronary and renal vasculatures and increased aortic blood flow, vertebral blood flow, coronary blood flow, peak positive left ventricular dP/dt and heart rate in anesthetized open-chest dogs. These cardiovascular effects of KT-1 were similar to those of glyceryl trinitrate (nitroglycerin, GTN). Nitrate-deleted KT-1 from its chemical structure (denitro KT-1) equimolar to KT-1 produced no marked changes in these cardiovascular parameters, but 3 or 10 times large doses of denitro KT-1 showed relatively long persisting vasodilator effects. In isolated dog coronary artery preparations contracted with KCl, the order of relaxant potency was GTN greater than KT-1 greater than denitro KT-1. In isolated dog mesenteric artery preparations, phenylephrine produced concentration-dependent contractions which were significantly inhibited by prazosin and KT-1 but not by denitro KT-1. In anesthetized open-chest dogs, phenylephrine produced pressor responses which were significantly inhibited by KT-1 but not by GTN or denitro KT-1. In isolated rat thoracic aorta strips, in contrast to GTN, KT-1 hardly developed a tachyphylaxis. Thus, KT-1 showed cardiovascular effects similar to those of both nitrates and a1-adrenoceptor blocking agents with no development of a tachyphylaxis. |
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Authors:
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Y Miyamoto; K Noguchi; J Nakasone; M Sakanashi |
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Publication Detail:
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Type: Comparative Study; In Vitro; Journal Article |
Journal Detail:
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Title: Arzneimittel-Forschung Volume: 41 ISSN: 0004-4172 ISO Abbreviation: Arzneimittelforschung Publication Date: 1991 Dec |
Date Detail:
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Created Date: 1992-06-23 Completed Date: 1992-06-23 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0372660 Medline TA: Arzneimittelforschung Country: GERMANY |
Other Details:
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Languages: eng Pagination: 1216-21 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, School of Medicine, Faculty of Medicine, University of the Ryukyus, Okinawa, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Aorta, Thoracic / drug effects Blood Pressure / drug effects Cardiovascular Agents / pharmacology* Cardiovascular System / drug effects* Coronary Vessels / drug effects Dogs Endothelium, Vascular / drug effects Female Heart Rate / drug effects Male Muscle, Smooth, Vascular / drug effects Nitro Compounds / pharmacology* Nitroglycerin / pharmacology Norepinephrine / pharmacology Phenylephrine / pharmacology Prazosin / pharmacology Quinazolines / pharmacology* Rats Rats, Inbred Strains Regional Blood Flow / drug effects Vascular Resistance / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Cardiovascular Agents; 0/Nitro Compounds; 0/Quinazolines; 19216-56-9/Prazosin; 33371-02-7/denitro-KT-1; 47487-05-8/KT 1; 51-41-2/Norepinephrine; 55-63-0/Nitroglycerin; 59-42-7/Phenylephrine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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