Dopamine DA1 receptor agonist activity of YM435 in the canine renal vasculature

1. The renal vasodilatory effect of YM435 was used as an index of its dopamine DA1 receptor agonist activity and compared with that of dopamine in pentobarbital-anesthetized dogs. 2. Intrarenal arterial administration of YM435 (0.1 to 10 micrograms) and dopamine (1 to 100 micrograms) produced a dose...

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Veröffentlicht in:General pharmacology 1997-08, Vol.29 (2), p.229-232
Hauptverfasser: YATSU, T, UCHIDA, W, INAGAKI, O, TANAKA, A, TAKENAKA, T
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container_end_page 232
container_issue 2
container_start_page 229
container_title General pharmacology
container_volume 29
creator YATSU, T
UCHIDA, W
INAGAKI, O
TANAKA, A
TAKENAKA, T
description 1. The renal vasodilatory effect of YM435 was used as an index of its dopamine DA1 receptor agonist activity and compared with that of dopamine in pentobarbital-anesthetized dogs. 2. Intrarenal arterial administration of YM435 (0.1 to 10 micrograms) and dopamine (1 to 100 micrograms) produced a dose-dependent increase in renal blood flow. The doses of YM435 and dopamine required to cause a 30-ml/min increase in renal blood flow were 2.0 and 26.8 micrograms intra-arterially (IA), respectively. YM435 was therefore 13 times more potent than dopamine in this effect. 3. The selective dopamine DA1 receptor antagonist, SCH 23390, but not the selective dopamine DA2 receptor antagonist, nemonapride, caused dose-dependent, parallel shifts to the right in the dose-responsive curve of YM435. 4. The present results demonstrate that YM435 is a potent and selective dopamine DA1 receptor agonist.
doi_str_mv 10.1016/S0306-3623(96)00402-8
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The renal vasodilatory effect of YM435 was used as an index of its dopamine DA1 receptor agonist activity and compared with that of dopamine in pentobarbital-anesthetized dogs. 2. Intrarenal arterial administration of YM435 (0.1 to 10 micrograms) and dopamine (1 to 100 micrograms) produced a dose-dependent increase in renal blood flow. The doses of YM435 and dopamine required to cause a 30-ml/min increase in renal blood flow were 2.0 and 26.8 micrograms intra-arterially (IA), respectively. YM435 was therefore 13 times more potent than dopamine in this effect. 3. The selective dopamine DA1 receptor antagonist, SCH 23390, but not the selective dopamine DA2 receptor antagonist, nemonapride, caused dose-dependent, parallel shifts to the right in the dose-responsive curve of YM435. 4. 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The renal vasodilatory effect of YM435 was used as an index of its dopamine DA1 receptor agonist activity and compared with that of dopamine in pentobarbital-anesthetized dogs. 2. Intrarenal arterial administration of YM435 (0.1 to 10 micrograms) and dopamine (1 to 100 micrograms) produced a dose-dependent increase in renal blood flow. The doses of YM435 and dopamine required to cause a 30-ml/min increase in renal blood flow were 2.0 and 26.8 micrograms intra-arterially (IA), respectively. YM435 was therefore 13 times more potent than dopamine in this effect. 3. The selective dopamine DA1 receptor antagonist, SCH 23390, but not the selective dopamine DA2 receptor antagonist, nemonapride, caused dose-dependent, parallel shifts to the right in the dose-responsive curve of YM435. 4. The present results demonstrate that YM435 is a potent and selective dopamine DA1 receptor agonist.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cardiovascular system</subject><subject>Dogs</subject><subject>Dopamine - pharmacology</subject><subject>Dopamine Agonists - pharmacology</subject><subject>Female</subject><subject>Fenoldopam - pharmacology</subject><subject>Isoquinolines - pharmacology</subject><subject>Kidney - blood supply</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Regional Blood Flow - drug effects</subject><subject>Tetrahydroisoquinolines</subject><subject>Vasodilator Agents - pharmacology</subject><subject>Vasodilator agents. 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Drug treatments</topic><topic>Regional Blood Flow - drug effects</topic><topic>Tetrahydroisoquinolines</topic><topic>Vasodilator Agents - pharmacology</topic><topic>Vasodilator agents. Cerebral vasodilators</topic><toplevel>online_resources</toplevel><creatorcontrib>YATSU, T</creatorcontrib><creatorcontrib>UCHIDA, W</creatorcontrib><creatorcontrib>INAGAKI, O</creatorcontrib><creatorcontrib>TANAKA, A</creatorcontrib><creatorcontrib>TAKENAKA, T</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>General pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>YATSU, T</au><au>UCHIDA, W</au><au>INAGAKI, O</au><au>TANAKA, A</au><au>TAKENAKA, T</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Dopamine DA1 receptor agonist activity of YM435 in the canine renal vasculature</atitle><jtitle>General pharmacology</jtitle><addtitle>Gen Pharmacol</addtitle><date>1997-08</date><risdate>1997</risdate><volume>29</volume><issue>2</issue><spage>229</spage><epage>232</epage><pages>229-232</pages><issn>0306-3623</issn><eissn>1879-0011</eissn><coden>GEPHDP</coden><abstract>1. The renal vasodilatory effect of YM435 was used as an index of its dopamine DA1 receptor agonist activity and compared with that of dopamine in pentobarbital-anesthetized dogs. 2. Intrarenal arterial administration of YM435 (0.1 to 10 micrograms) and dopamine (1 to 100 micrograms) produced a dose-dependent increase in renal blood flow. The doses of YM435 and dopamine required to cause a 30-ml/min increase in renal blood flow were 2.0 and 26.8 micrograms intra-arterially (IA), respectively. YM435 was therefore 13 times more potent than dopamine in this effect. 3. The selective dopamine DA1 receptor antagonist, SCH 23390, but not the selective dopamine DA2 receptor antagonist, nemonapride, caused dose-dependent, parallel shifts to the right in the dose-responsive curve of YM435. 4. The present results demonstrate that YM435 is a potent and selective dopamine DA1 receptor agonist.</abstract><cop>New York, NY</cop><pub>Elsevier</pub><pmid>9251904</pmid><doi>10.1016/S0306-3623(96)00402-8</doi><tpages>4</tpages></addata></record>
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subjects Animals
Biological and medical sciences
Cardiovascular system
Dogs
Dopamine - pharmacology
Dopamine Agonists - pharmacology
Female
Fenoldopam - pharmacology
Isoquinolines - pharmacology
Kidney - blood supply
Male
Medical sciences
Pharmacology. Drug treatments
Regional Blood Flow - drug effects
Tetrahydroisoquinolines
Vasodilator Agents - pharmacology
Vasodilator agents. Cerebral vasodilators
title Dopamine DA1 receptor agonist activity of YM435 in the canine renal vasculature
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