5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats
The present study was designed to investigate which subtype of spinal 5-HT receptors were involved in acetaminophen-induced antinociception using the paw-pressure test. Propacetamol (prodrug of acetaminophen, 400 mg/kg, injected intravenously, corresponding to 200 mg/kg of acetaminophen) produced a...
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Veröffentlicht in: | European journal of pharmacology 2001-11, Vol.432 (1), p.1-7 |
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description | The present study was designed to investigate which subtype of spinal 5-HT receptors were involved in acetaminophen-induced antinociception using the paw-pressure test. Propacetamol (prodrug of acetaminophen, 400 mg/kg, injected intravenously, corresponding to 200 mg/kg of acetaminophen) produced a significant antinociceptive effect in this test. This effect was at least partially inhibited by intrathecal (i.t.) pretreatment with the 5-HT
1B (penbutolol), 5-HT
2A (ketanserin), 5-HT
2C (mesulergine) receptor antagonists, but not by the 5-HT
1A (
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-
N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride, WAY 100635) and 5-HT
3 (granisetron) receptor antagonists. This profile was very close to that obtained recently with 5-HT, which suggests an implication of 5-HT in the spinal antinociceptive effect of acetaminophen. These results, the lack of binding of acetaminophen to 5-HT receptors and the increase of central 5-HT levels induced by this drug suggest that acetaminophen-induced antinociception could be indirectly mediated by 5-HT. |
doi_str_mv | 10.1016/S0014-2999(01)01464-9 |
format | Article |
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1B (penbutolol), 5-HT
2A (ketanserin), 5-HT
2C (mesulergine) receptor antagonists, but not by the 5-HT
1A (
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-
N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride, WAY 100635) and 5-HT
3 (granisetron) receptor antagonists. This profile was very close to that obtained recently with 5-HT, which suggests an implication of 5-HT in the spinal antinociceptive effect of acetaminophen. These results, the lack of binding of acetaminophen to 5-HT receptors and the increase of central 5-HT levels induced by this drug suggest that acetaminophen-induced antinociception could be indirectly mediated by 5-HT.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/S0014-2999(01)01464-9</identifier><identifier>PMID: 11734181</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>5-HT receptor antagonist ; Acetaminophen ; Acetaminophen - pharmacology ; Analgesics ; Analgesics - pharmacology ; Animals ; Antinociception ; Biological and medical sciences ; Ergolines - pharmacology ; Granisetron - pharmacology ; Injections, Spinal ; Ketanserin - pharmacology ; Male ; Medical sciences ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pain Threshold - drug effects ; Paw-pressure test ; Penbutolol - pharmacology ; Pharmacology. Drug treatments ; Piperazines - pharmacology ; Pyridines - pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptor, Serotonin, 5-HT1B ; Receptor, Serotonin, 5-HT2A ; Receptor, Serotonin, 5-HT2C ; Receptors, Serotonin - drug effects ; Receptors, Serotonin - physiology ; Receptors, Serotonin, 5-HT1 ; Receptors, Serotonin, 5-HT3 ; Serotonin Antagonists - pharmacology ; Serotoninergic system ; Time Factors ; Vocalization, Animal - drug effects</subject><ispartof>European journal of pharmacology, 2001-11, Vol.432 (1), p.1-7</ispartof><rights>2001 Elsevier Science B.V.</rights><rights>2002 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c457t-64b3187ea739106bf772bd3fe29c618bcf81606e289f59bb17206fa05bb91e9f3</citedby><cites>FETCH-LOGICAL-c457t-64b3187ea739106bf772bd3fe29c618bcf81606e289f59bb17206fa05bb91e9f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0014-2999(01)01464-9$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,778,782,3539,27907,27908,45978</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=13378004$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11734181$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Courade, Jean-Philippe</creatorcontrib><creatorcontrib>Chassaing, Claude</creatorcontrib><creatorcontrib>Bardin, Laurent</creatorcontrib><creatorcontrib>Alloui, Abdelkrim</creatorcontrib><creatorcontrib>Eschalier, Alain</creatorcontrib><title>5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>The present study was designed to investigate which subtype of spinal 5-HT receptors were involved in acetaminophen-induced antinociception using the paw-pressure test. Propacetamol (prodrug of acetaminophen, 400 mg/kg, injected intravenously, corresponding to 200 mg/kg of acetaminophen) produced a significant antinociceptive effect in this test. This effect was at least partially inhibited by intrathecal (i.t.) pretreatment with the 5-HT
1B (penbutolol), 5-HT
2A (ketanserin), 5-HT
2C (mesulergine) receptor antagonists, but not by the 5-HT
1A (
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-
N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride, WAY 100635) and 5-HT
3 (granisetron) receptor antagonists. This profile was very close to that obtained recently with 5-HT, which suggests an implication of 5-HT in the spinal antinociceptive effect of acetaminophen. These results, the lack of binding of acetaminophen to 5-HT receptors and the increase of central 5-HT levels induced by this drug suggest that acetaminophen-induced antinociception could be indirectly mediated by 5-HT.</description><subject>5-HT receptor antagonist</subject><subject>Acetaminophen</subject><subject>Acetaminophen - pharmacology</subject><subject>Analgesics</subject><subject>Analgesics - pharmacology</subject><subject>Animals</subject><subject>Antinociception</subject><subject>Biological and medical sciences</subject><subject>Ergolines - pharmacology</subject><subject>Granisetron - pharmacology</subject><subject>Injections, Spinal</subject><subject>Ketanserin - pharmacology</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pain Threshold - drug effects</subject><subject>Paw-pressure test</subject><subject>Penbutolol - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperazines - pharmacology</subject><subject>Pyridines - pharmacology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptor, Serotonin, 5-HT1B</subject><subject>Receptor, Serotonin, 5-HT2A</subject><subject>Receptor, Serotonin, 5-HT2C</subject><subject>Receptors, Serotonin - drug effects</subject><subject>Receptors, Serotonin - physiology</subject><subject>Receptors, Serotonin, 5-HT1</subject><subject>Receptors, Serotonin, 5-HT3</subject><subject>Serotonin Antagonists - pharmacology</subject><subject>Serotoninergic system</subject><subject>Time Factors</subject><subject>Vocalization, Animal - drug effects</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkcFu1DAQhi0EotvCI4B8AcEhMOMkdnxCqKIUqRIHyhFZtjNWjbJJsL0r9e3xdlf0yMkj-ftnRt8w9grhAwLKjz8AsGuE1vod4Ptay67RT9gGB6UbUCiess0_5Iyd5_wbAHot-ufsDFG1HQ64Yb_65vqWJ_K0liXxvHPlfqXM47xfpj2NteDljnhe42wnbucS58XHAx73xCkE8oUvgVtPxW7r53pH8yGVbMkv2LNgp0wvT-8F-3n15fbyurn5_vXb5eebxne9Ko3sXFv3JqtajSBdUEq4sQ0ktJc4OB8GlCBJDDr02jlUAmSw0DunkXRoL9jbY981LX92lIvZxuxpmuxMyy4bJVqhtOwr2B9Bn5acEwWzpri16d4gmINX8-DVHKQZQPPg1eiae30asHNbGh9TJ5EVeHMCbPZ2CsnOPuZHrm3VANBV7tORo6pjHymZ7CPNnsZYj1DMuMT_rPIX_emU5Q</recordid><startdate>20011130</startdate><enddate>20011130</enddate><creator>Courade, Jean-Philippe</creator><creator>Chassaing, Claude</creator><creator>Bardin, Laurent</creator><creator>Alloui, Abdelkrim</creator><creator>Eschalier, Alain</creator><general>Elsevier B.V</general><general>Elsevier</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>7X8</scope></search><sort><creationdate>20011130</creationdate><title>5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats</title><author>Courade, Jean-Philippe ; Chassaing, Claude ; Bardin, Laurent ; Alloui, Abdelkrim ; Eschalier, Alain</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c457t-64b3187ea739106bf772bd3fe29c618bcf81606e289f59bb17206fa05bb91e9f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>5-HT receptor antagonist</topic><topic>Acetaminophen</topic><topic>Acetaminophen - pharmacology</topic><topic>Analgesics</topic><topic>Analgesics - pharmacology</topic><topic>Animals</topic><topic>Antinociception</topic><topic>Biological and medical sciences</topic><topic>Ergolines - pharmacology</topic><topic>Granisetron - pharmacology</topic><topic>Injections, Spinal</topic><topic>Ketanserin - pharmacology</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pain Threshold - drug effects</topic><topic>Paw-pressure test</topic><topic>Penbutolol - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperazines - pharmacology</topic><topic>Pyridines - pharmacology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptor, Serotonin, 5-HT1B</topic><topic>Receptor, Serotonin, 5-HT2A</topic><topic>Receptor, Serotonin, 5-HT2C</topic><topic>Receptors, Serotonin - drug effects</topic><topic>Receptors, Serotonin - physiology</topic><topic>Receptors, Serotonin, 5-HT1</topic><topic>Receptors, Serotonin, 5-HT3</topic><topic>Serotonin Antagonists - pharmacology</topic><topic>Serotoninergic system</topic><topic>Time Factors</topic><topic>Vocalization, Animal - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Courade, Jean-Philippe</creatorcontrib><creatorcontrib>Chassaing, Claude</creatorcontrib><creatorcontrib>Bardin, Laurent</creatorcontrib><creatorcontrib>Alloui, Abdelkrim</creatorcontrib><creatorcontrib>Eschalier, Alain</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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Courade, Jean-Philippe</au><au>Chassaing, Claude</au><au>Bardin, Laurent</au><au>Alloui, Abdelkrim</au><au>Eschalier, Alain</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>2001-11-30</date><risdate>2001</risdate><volume>432</volume><issue>1</issue><spage>1</spage><epage>7</epage><pages>1-7</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The present study was designed to investigate which subtype of spinal 5-HT receptors were involved in acetaminophen-induced antinociception using the paw-pressure test. Propacetamol (prodrug of acetaminophen, 400 mg/kg, injected intravenously, corresponding to 200 mg/kg of acetaminophen) produced a significant antinociceptive effect in this test. This effect was at least partially inhibited by intrathecal (i.t.) pretreatment with the 5-HT
1B (penbutolol), 5-HT
2A (ketanserin), 5-HT
2C (mesulergine) receptor antagonists, but not by the 5-HT
1A (
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-
N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride, WAY 100635) and 5-HT
3 (granisetron) receptor antagonists. This profile was very close to that obtained recently with 5-HT, which suggests an implication of 5-HT in the spinal antinociceptive effect of acetaminophen. These results, the lack of binding of acetaminophen to 5-HT receptors and the increase of central 5-HT levels induced by this drug suggest that acetaminophen-induced antinociception could be indirectly mediated by 5-HT.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>11734181</pmid><doi>10.1016/S0014-2999(01)01464-9</doi><tpages>7</tpages></addata></record> |
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subjects | 5-HT receptor antagonist Acetaminophen Acetaminophen - pharmacology Analgesics Analgesics - pharmacology Animals Antinociception Biological and medical sciences Ergolines - pharmacology Granisetron - pharmacology Injections, Spinal Ketanserin - pharmacology Male Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pain Threshold - drug effects Paw-pressure test Penbutolol - pharmacology Pharmacology. Drug treatments Piperazines - pharmacology Pyridines - pharmacology Rats Rats, Sprague-Dawley Receptor, Serotonin, 5-HT1B Receptor, Serotonin, 5-HT2A Receptor, Serotonin, 5-HT2C Receptors, Serotonin - drug effects Receptors, Serotonin - physiology Receptors, Serotonin, 5-HT1 Receptors, Serotonin, 5-HT3 Serotonin Antagonists - pharmacology Serotoninergic system Time Factors Vocalization, Animal - drug effects |
title | 5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats |
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