Inhibitory effect of tramadol on vasorelaxation mediated by ATP-sensitive K+ channels in rat aorta
Tramadol produces a conduction block similar to lidocaine by exerting a local anesthetic-like effect. The aims of this in vitro study were to determine the effects of tramadol on the vasorelaxant response induced by the adenosine triphosphate-sensitive K(+) (K(ATP)) channel opener, levcromakalim, in...
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| Veröffentlicht in: | Canadian journal of anesthesia 2007-06, Vol.54 (6), p.453-460 |
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| creator | CHO, Hyoung-Chan SOHN, Ju-Tae PARK, Kyeong-Eon SHIN, Il-Woo KI CHURL CHANG LEE, Jae-Wan LEE, Heon-Keun CHUNG, Young-Kyun |
| description | Tramadol produces a conduction block similar to lidocaine by exerting a local anesthetic-like effect. The aims of this in vitro study were to determine the effects of tramadol on the vasorelaxant response induced by the adenosine triphosphate-sensitive K(+) (K(ATP)) channel opener, levcromakalim, in an endothelium-denuded rat aorta, and to determine whether this effect of tramadol is stereoselective.
The effects of tramadol (racemic, R(-) and S(+): 10(-6), 10(-5), 5 x 10(-5) M), and glibenclamide on the levcromakalim dose-response curve were assessed in aortic rings that had been pre-contracted with phenylephrine. In the rings pretreated independently with naloxone, and glibenclamide, the levcromakalim dose-response curves were generated in the presence or absence of tramadol. The effect of tramadol on the dose-response curve of diltiazem was assessed.
Racemic, R(-) and S(+) tramadol (10(-5), 5 x 10(-5) M) attenuated (P < 0.0001) levcromakalim-induced relaxation in the ring with or without naloxone in a dose-dependent manner. The magnitude of the R(-)-tramadol-induced attenuation of vasorelaxant response induced by levcromakalim was greater (P < 0.05) than that induced by S(+)-tramadol. Glibenclamide almost abolished the levcromakalim-induced relaxation. Tramadol, 5 x 10(-5) M, did not significantly alter the diltiazem-induced relaxation.
These results suggest that a supraclinical dose (10(-5) M) of tramadol [racemic, R(-) and S(+)] attenuates the vasorelaxation mediated by the K(ATP) channels in the rat aorta. The R(-) tramadol-induced attenuation of vasorelaxation induced by levcromaklim was more potent than that induced by S(+) tramadol. This attenuation is independent of opioid receptor activation. |
| doi_str_mv | 10.1007/BF03022031 |
| format | Article |
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The effects of tramadol (racemic, R(-) and S(+): 10(-6), 10(-5), 5 x 10(-5) M), and glibenclamide on the levcromakalim dose-response curve were assessed in aortic rings that had been pre-contracted with phenylephrine. In the rings pretreated independently with naloxone, and glibenclamide, the levcromakalim dose-response curves were generated in the presence or absence of tramadol. The effect of tramadol on the dose-response curve of diltiazem was assessed.
Racemic, R(-) and S(+) tramadol (10(-5), 5 x 10(-5) M) attenuated (P < 0.0001) levcromakalim-induced relaxation in the ring with or without naloxone in a dose-dependent manner. The magnitude of the R(-)-tramadol-induced attenuation of vasorelaxant response induced by levcromakalim was greater (P < 0.05) than that induced by S(+)-tramadol. Glibenclamide almost abolished the levcromakalim-induced relaxation. Tramadol, 5 x 10(-5) M, did not significantly alter the diltiazem-induced relaxation.
These results suggest that a supraclinical dose (10(-5) M) of tramadol [racemic, R(-) and S(+)] attenuates the vasorelaxation mediated by the K(ATP) channels in the rat aorta. The R(-) tramadol-induced attenuation of vasorelaxation induced by levcromaklim was more potent than that induced by S(+) tramadol. This attenuation is independent of opioid receptor activation.</description><identifier>ISSN: 0832-610X</identifier><identifier>EISSN: 1496-8975</identifier><identifier>DOI: 10.1007/BF03022031</identifier><identifier>PMID: 17541074</identifier><identifier>CODEN: CJOAEP</identifier><language>eng</language><publisher>Toronto, ON: Canadian Anesthesiologists' Society</publisher><subject>Analgesics, Opioid - chemistry ; Analgesics, Opioid - pharmacology ; Anesthesia ; Anesthesia. Intensive care medicine. Transfusions. Cell therapy and gene therapy ; Animals ; Aorta - drug effects ; Biological and medical sciences ; Calcium Channel Blockers - pharmacology ; Cromakalim - pharmacology ; Data Interpretation, Statistical ; Diltiazem - pharmacology ; Dose-Response Relationship, Drug ; Glyburide - pharmacology ; Hypoglycemic Agents - pharmacology ; In Vitro Techniques ; KATP Channels ; Male ; Medical sciences ; Muscle Relaxation - drug effects ; Muscle, Smooth, Vascular - drug effects ; Potassium Channel Blockers - pharmacology ; Potassium Channels, Inwardly Rectifying - drug effects ; Potassium Channels, Inwardly Rectifying - physiology ; Rats ; Rats, Sprague-Dawley ; Rodents ; Stereoisomerism ; Tramadol - chemistry ; Tramadol - pharmacology</subject><ispartof>Canadian journal of anesthesia, 2007-06, Vol.54 (6), p.453-460</ispartof><rights>2007 INIST-CNRS</rights><rights>Canadian Anesthesiologists 2007</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c378t-71f2f9e2f52670fa079866e645ed96858a5e3fb2006148e1ab53f7a11e37ece03</citedby><cites>FETCH-LOGICAL-c378t-71f2f9e2f52670fa079866e645ed96858a5e3fb2006148e1ab53f7a11e37ece03</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18826065$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17541074$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>CHO, Hyoung-Chan</creatorcontrib><creatorcontrib>SOHN, Ju-Tae</creatorcontrib><creatorcontrib>PARK, Kyeong-Eon</creatorcontrib><creatorcontrib>SHIN, Il-Woo</creatorcontrib><creatorcontrib>KI CHURL CHANG</creatorcontrib><creatorcontrib>LEE, Jae-Wan</creatorcontrib><creatorcontrib>LEE, Heon-Keun</creatorcontrib><creatorcontrib>CHUNG, Young-Kyun</creatorcontrib><title>Inhibitory effect of tramadol on vasorelaxation mediated by ATP-sensitive K+ channels in rat aorta</title><title>Canadian journal of anesthesia</title><addtitle>Can J Anaesth</addtitle><description>Tramadol produces a conduction block similar to lidocaine by exerting a local anesthetic-like effect. The aims of this in vitro study were to determine the effects of tramadol on the vasorelaxant response induced by the adenosine triphosphate-sensitive K(+) (K(ATP)) channel opener, levcromakalim, in an endothelium-denuded rat aorta, and to determine whether this effect of tramadol is stereoselective.
The effects of tramadol (racemic, R(-) and S(+): 10(-6), 10(-5), 5 x 10(-5) M), and glibenclamide on the levcromakalim dose-response curve were assessed in aortic rings that had been pre-contracted with phenylephrine. In the rings pretreated independently with naloxone, and glibenclamide, the levcromakalim dose-response curves were generated in the presence or absence of tramadol. The effect of tramadol on the dose-response curve of diltiazem was assessed.
Racemic, R(-) and S(+) tramadol (10(-5), 5 x 10(-5) M) attenuated (P < 0.0001) levcromakalim-induced relaxation in the ring with or without naloxone in a dose-dependent manner. The magnitude of the R(-)-tramadol-induced attenuation of vasorelaxant response induced by levcromakalim was greater (P < 0.05) than that induced by S(+)-tramadol. Glibenclamide almost abolished the levcromakalim-induced relaxation. Tramadol, 5 x 10(-5) M, did not significantly alter the diltiazem-induced relaxation.
These results suggest that a supraclinical dose (10(-5) M) of tramadol [racemic, R(-) and S(+)] attenuates the vasorelaxation mediated by the K(ATP) channels in the rat aorta. The R(-) tramadol-induced attenuation of vasorelaxation induced by levcromaklim was more potent than that induced by S(+) tramadol. This attenuation is independent of opioid receptor activation.</description><subject>Analgesics, Opioid - chemistry</subject><subject>Analgesics, Opioid - pharmacology</subject><subject>Anesthesia</subject><subject>Anesthesia. Intensive care medicine. Transfusions. Cell therapy and gene therapy</subject><subject>Animals</subject><subject>Aorta - drug effects</subject><subject>Biological and medical sciences</subject><subject>Calcium Channel Blockers - pharmacology</subject><subject>Cromakalim - pharmacology</subject><subject>Data Interpretation, Statistical</subject><subject>Diltiazem - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>Glyburide - pharmacology</subject><subject>Hypoglycemic Agents - pharmacology</subject><subject>In Vitro Techniques</subject><subject>KATP Channels</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Muscle Relaxation - drug effects</subject><subject>Muscle, Smooth, Vascular - drug effects</subject><subject>Potassium Channel Blockers - pharmacology</subject><subject>Potassium Channels, Inwardly Rectifying - drug effects</subject><subject>Potassium Channels, Inwardly Rectifying - physiology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Rodents</subject><subject>Stereoisomerism</subject><subject>Tramadol - chemistry</subject><subject>Tramadol - pharmacology</subject><issn>0832-610X</issn><issn>1496-8975</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><recordid>eNpd0N9LHDEQwPEgLXpqX_wDJBT0oWXbSbL5sY8qtZUK9cFC35bZvQlG9hKb5KT337viwUGfhoEPw_Bl7ETAFwFgv15egwIpQYk9thBtZxrXWf2OLcAp2RgBfw7YYSmPAOCMdvvsQFjdCrDtgg038SEMoaa84eQ9jZUnz2vGFS7TxFPkz1hSpgn_YQ3zuqJlwEpLPmz4xf1dUyiWUMMz8Z-f-fiAMdJUeIg8Y-WYcsVj9t7jVOjDdh6x39ff7q9-NLe_vt9cXdw2o7KuNlZ46TuSXktjwSPYzhlDptW07IzTDjUpP0gAI1pHAgetvEUhSFkaCdQRO3-7-5TT3zWV2q9CGWmaMFJal96CNmbuNcOP_8HHtM5x_q13ToNshXtFn97QmFMpmXz_lMMK86YX0L9m73fZZ3y6vbge5kA7uu08g7MtwDLi5DPGMZSdc04aMFq9AG_SiG4</recordid><startdate>20070601</startdate><enddate>20070601</enddate><creator>CHO, Hyoung-Chan</creator><creator>SOHN, Ju-Tae</creator><creator>PARK, Kyeong-Eon</creator><creator>SHIN, Il-Woo</creator><creator>KI CHURL CHANG</creator><creator>LEE, Jae-Wan</creator><creator>LEE, Heon-Keun</creator><creator>CHUNG, Young-Kyun</creator><general>Canadian Anesthesiologists' Society</general><general>Springer Nature B.V</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7RV</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>8FQ</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>K9.</scope><scope>KB0</scope><scope>M0S</scope><scope>M1P</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope><scope>7X8</scope></search><sort><creationdate>20070601</creationdate><title>Inhibitory effect of tramadol on vasorelaxation mediated by ATP-sensitive K+ channels in rat aorta</title><author>CHO, Hyoung-Chan ; SOHN, Ju-Tae ; PARK, Kyeong-Eon ; SHIN, Il-Woo ; KI CHURL CHANG ; LEE, Jae-Wan ; LEE, Heon-Keun ; CHUNG, Young-Kyun</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c378t-71f2f9e2f52670fa079866e645ed96858a5e3fb2006148e1ab53f7a11e37ece03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Analgesics, Opioid - chemistry</topic><topic>Analgesics, Opioid - pharmacology</topic><topic>Anesthesia</topic><topic>Anesthesia. Intensive care medicine. Transfusions. Cell therapy and gene therapy</topic><topic>Animals</topic><topic>Aorta - drug effects</topic><topic>Biological and medical sciences</topic><topic>Calcium Channel Blockers - pharmacology</topic><topic>Cromakalim - pharmacology</topic><topic>Data Interpretation, Statistical</topic><topic>Diltiazem - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>Glyburide - pharmacology</topic><topic>Hypoglycemic Agents - pharmacology</topic><topic>In Vitro Techniques</topic><topic>KATP Channels</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Muscle Relaxation - drug effects</topic><topic>Muscle, Smooth, Vascular - drug effects</topic><topic>Potassium Channel Blockers - pharmacology</topic><topic>Potassium Channels, Inwardly Rectifying - drug effects</topic><topic>Potassium Channels, Inwardly Rectifying - physiology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Rodents</topic><topic>Stereoisomerism</topic><topic>Tramadol - chemistry</topic><topic>Tramadol - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>CHO, Hyoung-Chan</creatorcontrib><creatorcontrib>SOHN, Ju-Tae</creatorcontrib><creatorcontrib>PARK, Kyeong-Eon</creatorcontrib><creatorcontrib>SHIN, Il-Woo</creatorcontrib><creatorcontrib>KI CHURL CHANG</creatorcontrib><creatorcontrib>LEE, Jae-Wan</creatorcontrib><creatorcontrib>LEE, Heon-Keun</creatorcontrib><creatorcontrib>CHUNG, Young-Kyun</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>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Canadian Business & Current Affairs Database</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>ProQuest Central Basic</collection><collection>MEDLINE - Academic</collection><jtitle>Canadian journal of anesthesia</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>CHO, Hyoung-Chan</au><au>SOHN, Ju-Tae</au><au>PARK, Kyeong-Eon</au><au>SHIN, Il-Woo</au><au>KI CHURL CHANG</au><au>LEE, Jae-Wan</au><au>LEE, Heon-Keun</au><au>CHUNG, Young-Kyun</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibitory effect of tramadol on vasorelaxation mediated by ATP-sensitive K+ channels in rat aorta</atitle><jtitle>Canadian journal of anesthesia</jtitle><addtitle>Can J Anaesth</addtitle><date>2007-06-01</date><risdate>2007</risdate><volume>54</volume><issue>6</issue><spage>453</spage><epage>460</epage><pages>453-460</pages><issn>0832-610X</issn><eissn>1496-8975</eissn><coden>CJOAEP</coden><abstract>Tramadol produces a conduction block similar to lidocaine by exerting a local anesthetic-like effect. The aims of this in vitro study were to determine the effects of tramadol on the vasorelaxant response induced by the adenosine triphosphate-sensitive K(+) (K(ATP)) channel opener, levcromakalim, in an endothelium-denuded rat aorta, and to determine whether this effect of tramadol is stereoselective.
The effects of tramadol (racemic, R(-) and S(+): 10(-6), 10(-5), 5 x 10(-5) M), and glibenclamide on the levcromakalim dose-response curve were assessed in aortic rings that had been pre-contracted with phenylephrine. In the rings pretreated independently with naloxone, and glibenclamide, the levcromakalim dose-response curves were generated in the presence or absence of tramadol. The effect of tramadol on the dose-response curve of diltiazem was assessed.
Racemic, R(-) and S(+) tramadol (10(-5), 5 x 10(-5) M) attenuated (P < 0.0001) levcromakalim-induced relaxation in the ring with or without naloxone in a dose-dependent manner. The magnitude of the R(-)-tramadol-induced attenuation of vasorelaxant response induced by levcromakalim was greater (P < 0.05) than that induced by S(+)-tramadol. Glibenclamide almost abolished the levcromakalim-induced relaxation. Tramadol, 5 x 10(-5) M, did not significantly alter the diltiazem-induced relaxation.
These results suggest that a supraclinical dose (10(-5) M) of tramadol [racemic, R(-) and S(+)] attenuates the vasorelaxation mediated by the K(ATP) channels in the rat aorta. The R(-) tramadol-induced attenuation of vasorelaxation induced by levcromaklim was more potent than that induced by S(+) tramadol. This attenuation is independent of opioid receptor activation.</abstract><cop>Toronto, ON</cop><pub>Canadian Anesthesiologists' Society</pub><pmid>17541074</pmid><doi>10.1007/BF03022031</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Canadian journal of anesthesia, 2007-06, Vol.54 (6), p.453-460 |
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| subjects | Analgesics, Opioid - chemistry Analgesics, Opioid - pharmacology Anesthesia Anesthesia. Intensive care medicine. Transfusions. Cell therapy and gene therapy Animals Aorta - drug effects Biological and medical sciences Calcium Channel Blockers - pharmacology Cromakalim - pharmacology Data Interpretation, Statistical Diltiazem - pharmacology Dose-Response Relationship, Drug Glyburide - pharmacology Hypoglycemic Agents - pharmacology In Vitro Techniques KATP Channels Male Medical sciences Muscle Relaxation - drug effects Muscle, Smooth, Vascular - drug effects Potassium Channel Blockers - pharmacology Potassium Channels, Inwardly Rectifying - drug effects Potassium Channels, Inwardly Rectifying - physiology Rats Rats, Sprague-Dawley Rodents Stereoisomerism Tramadol - chemistry Tramadol - pharmacology |
| title | Inhibitory effect of tramadol on vasorelaxation mediated by ATP-sensitive K+ channels in rat aorta |
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