Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anesthetized rat
The effect of fedotozine was evaluated in a model of colonic hypersensibility to balloon distension in anesthetized rats. Acetic acid (0.6%, intracolonically) significantly enhanced the hypotension reflex response to colonic distension ( P
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| Veröffentlicht in: | European journal of pharmacology 1994-12, Vol.271 (2), p.245-251 |
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| creator | Langlois, Annik Diop, Laurent Rivière, Pierre J.M. Pascaud, Xavier Junien, Jean-Louis |
| description | The effect of fedotozine was evaluated in a model of colonic hypersensibility to balloon distension in anesthetized rats. Acetic acid (0.6%, intracolonically) significantly enhanced the hypotension reflex response to colonic distension (
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| doi_str_mv | 10.1016/0014-2999(94)90780-3 |
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| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_77799336</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>0014299994907803</els_id><sourcerecordid>16713349</sourcerecordid><originalsourceid>FETCH-LOGICAL-c417t-baa3834238cfca4a9bbf16b7566c027c869337ec19f57f69409b9a18175dbbfb3</originalsourceid><addsrcrecordid>eNqFUctq3DAUFaUhmaT9gwa0KKVZOJUs2bI2gRKStBDIJlkLWZboLR5rKskhj5_vdWeYZbO6cM-DwzmEfOLsnDPefmOMy6rWWn_V8kwz1bFKvCMr3ildMcXr92S1pxyR45x_M8YaXTeH5FAp1sharsjrVQjeFRoDDX6IJb7A5GmcaPnlqbNpgPhos5tHm-jGwkSTD6N_ojANs_MD7Z_pALn4KQOK0GXRQUpQbEHYxRHfsLWzk894C7wgkmz5QA6CHbP_uLsn5OH66v7yR3V7d_Pz8vtt5SRXpeqtFZ2QtehccFZa3feBt71q2taxWrmu1UIo77gOjQqtlkz32vKOq2ZAai9OyJet7ybFPzNmMGvIzo8jBopzNkopjRbtm0TeKi6E1EiUW6JLMWesxGwSrG16NpyZZRyzNG-W5o2W5t84RqDsdOc_92s_7EW7NRD_vMOxcjuGZCcHeU8TQivOl5gXW5rH0h7BJ5Md-AnngIRbmiHC_3P8BfBjrJU</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>16713349</pqid></control><display><type>article</type><title>Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anesthetized rat</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals Complete</source><creator>Langlois, Annik ; Diop, Laurent ; Rivière, Pierre J.M. ; Pascaud, Xavier ; Junien, Jean-Louis</creator><creatorcontrib>Langlois, Annik ; Diop, Laurent ; Rivière, Pierre J.M. ; Pascaud, Xavier ; Junien, Jean-Louis</creatorcontrib><description>The effect of fedotozine was evaluated in a model of colonic hypersensibility to balloon distension in anesthetized rats. Acetic acid (0.6%, intracolonically) significantly enhanced the hypotension reflex response to colonic distension (
P<0.05). At a noxious pain pressure (75 mm Hg), fedotozine ((+)-(−1
R)-1-phenyl-1-[(3,4,5-trimethoxy)benzyloxymethyl]-
N,
N-dimethyl-
n-propylamine) had no effect at 0.6 and 1 mg/kg i.v. in saline-treated rats and higher doses were required to produce antinociception (ED
50 = 2.57 mg/kg i.v.). By contrast, fedotozine at 0.6 and 1 mg/kg i.v. displayed 38 and 54% antinociception (
P < 0.05) respectively, in acetic acid-treated animals, leading to a decrease in its ED
50 (1.15 mg/kg i.v.). Similar results were obtained with (±)-
trans-
N-methyl-
N-[2-(pyrrolidinyl)-cyclohexyl]benzo[
b]-thiophene-4-acetamide (PD-117,302), a κ-opioid receptor agonist, while the antinociceptive action of morphine and a κ-opioid receptor agonist,
trans-(±)-3,4-dichloro-
N-methyl-
N-(2-[1-pyrrolidinyl] cyclohexyl)benzenacetamide ((±)-U-50,488H), was identical in control and acetic-treated animals. Nor-binaltorphimine, a selective κ-opioid receptor antagonist, reversed the enhanced antinociceptive activity of fedotozine and PD-117,302. It is concluded that acetic acid induces colonic hypersensibility to painful mechanical stimuli and that some but not all κ-opioid receptor ligands can have enhanced efficacy in this pathological situation.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(94)90780-3</identifier><identifier>PMID: 7705424</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer ; Acetates ; Acetic Acid ; Amino Acid Sequence ; Analgesics ; Anesthesia ; Animals ; Benzyl Compounds - pharmacology ; Biological and medical sciences ; Blood Pressure - drug effects ; Colon - drug effects ; Colon - physiology ; Colonic hypersensitivity ; Dose-Response Relationship, Drug ; Fedotozine ; Male ; Medical sciences ; Molecular Sequence Data ; Neuropharmacology ; Pain - physiopathology ; Pharmacology. Drug treatments ; Propylamines - pharmacology ; Pyrroles - pharmacology ; Pyrrolidines - pharmacology ; Rats ; Rats, Sprague-Dawley ; Reflex - drug effects ; Thiophenes - pharmacology ; Visceral pain ; κ-Opioid receptor ; μ-Opioid receptor</subject><ispartof>European journal of pharmacology, 1994-12, Vol.271 (2), p.245-251</ispartof><rights>1994</rights><rights>1995 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c417t-baa3834238cfca4a9bbf16b7566c027c869337ec19f57f69409b9a18175dbbfb3</citedby><cites>FETCH-LOGICAL-c417t-baa3834238cfca4a9bbf16b7566c027c869337ec19f57f69409b9a18175dbbfb3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0014-2999(94)90780-3$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3397116$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7705424$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Langlois, Annik</creatorcontrib><creatorcontrib>Diop, Laurent</creatorcontrib><creatorcontrib>Rivière, Pierre J.M.</creatorcontrib><creatorcontrib>Pascaud, Xavier</creatorcontrib><creatorcontrib>Junien, Jean-Louis</creatorcontrib><title>Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anesthetized rat</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>The effect of fedotozine was evaluated in a model of colonic hypersensibility to balloon distension in anesthetized rats. Acetic acid (0.6%, intracolonically) significantly enhanced the hypotension reflex response to colonic distension (
P<0.05). At a noxious pain pressure (75 mm Hg), fedotozine ((+)-(−1
R)-1-phenyl-1-[(3,4,5-trimethoxy)benzyloxymethyl]-
N,
N-dimethyl-
n-propylamine) had no effect at 0.6 and 1 mg/kg i.v. in saline-treated rats and higher doses were required to produce antinociception (ED
50 = 2.57 mg/kg i.v.). By contrast, fedotozine at 0.6 and 1 mg/kg i.v. displayed 38 and 54% antinociception (
P < 0.05) respectively, in acetic acid-treated animals, leading to a decrease in its ED
50 (1.15 mg/kg i.v.). Similar results were obtained with (±)-
trans-
N-methyl-
N-[2-(pyrrolidinyl)-cyclohexyl]benzo[
b]-thiophene-4-acetamide (PD-117,302), a κ-opioid receptor agonist, while the antinociceptive action of morphine and a κ-opioid receptor agonist,
trans-(±)-3,4-dichloro-
N-methyl-
N-(2-[1-pyrrolidinyl] cyclohexyl)benzenacetamide ((±)-U-50,488H), was identical in control and acetic-treated animals. Nor-binaltorphimine, a selective κ-opioid receptor antagonist, reversed the enhanced antinociceptive activity of fedotozine and PD-117,302. It is concluded that acetic acid induces colonic hypersensibility to painful mechanical stimuli and that some but not all κ-opioid receptor ligands can have enhanced efficacy in this pathological situation.</description><subject>3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer</subject><subject>Acetates</subject><subject>Acetic Acid</subject><subject>Amino Acid Sequence</subject><subject>Analgesics</subject><subject>Anesthesia</subject><subject>Animals</subject><subject>Benzyl Compounds - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Blood Pressure - drug effects</subject><subject>Colon - drug effects</subject><subject>Colon - physiology</subject><subject>Colonic hypersensitivity</subject><subject>Dose-Response Relationship, Drug</subject><subject>Fedotozine</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Molecular Sequence Data</subject><subject>Neuropharmacology</subject><subject>Pain - physiopathology</subject><subject>Pharmacology. Drug treatments</subject><subject>Propylamines - pharmacology</subject><subject>Pyrroles - pharmacology</subject><subject>Pyrrolidines - pharmacology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Reflex - drug effects</subject><subject>Thiophenes - pharmacology</subject><subject>Visceral pain</subject><subject>κ-Opioid receptor</subject><subject>μ-Opioid receptor</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFUctq3DAUFaUhmaT9gwa0KKVZOJUs2bI2gRKStBDIJlkLWZboLR5rKskhj5_vdWeYZbO6cM-DwzmEfOLsnDPefmOMy6rWWn_V8kwz1bFKvCMr3ildMcXr92S1pxyR45x_M8YaXTeH5FAp1sharsjrVQjeFRoDDX6IJb7A5GmcaPnlqbNpgPhos5tHm-jGwkSTD6N_ojANs_MD7Z_pALn4KQOK0GXRQUpQbEHYxRHfsLWzk894C7wgkmz5QA6CHbP_uLsn5OH66v7yR3V7d_Pz8vtt5SRXpeqtFZ2QtehccFZa3feBt71q2taxWrmu1UIo77gOjQqtlkz32vKOq2ZAai9OyJet7ybFPzNmMGvIzo8jBopzNkopjRbtm0TeKi6E1EiUW6JLMWesxGwSrG16NpyZZRyzNG-W5o2W5t84RqDsdOc_92s_7EW7NRD_vMOxcjuGZCcHeU8TQivOl5gXW5rH0h7BJ5Md-AnngIRbmiHC_3P8BfBjrJU</recordid><startdate>19941227</startdate><enddate>19941227</enddate><creator>Langlois, Annik</creator><creator>Diop, Laurent</creator><creator>Rivière, Pierre J.M.</creator><creator>Pascaud, Xavier</creator><creator>Junien, Jean-Louis</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>7TK</scope><scope>7X8</scope></search><sort><creationdate>19941227</creationdate><title>Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anesthetized rat</title><author>Langlois, Annik ; Diop, Laurent ; Rivière, Pierre J.M. ; Pascaud, Xavier ; Junien, Jean-Louis</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c417t-baa3834238cfca4a9bbf16b7566c027c869337ec19f57f69409b9a18175dbbfb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer</topic><topic>Acetates</topic><topic>Acetic Acid</topic><topic>Amino Acid Sequence</topic><topic>Analgesics</topic><topic>Anesthesia</topic><topic>Animals</topic><topic>Benzyl Compounds - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Blood Pressure - drug effects</topic><topic>Colon - drug effects</topic><topic>Colon - physiology</topic><topic>Colonic hypersensitivity</topic><topic>Dose-Response Relationship, Drug</topic><topic>Fedotozine</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Molecular Sequence Data</topic><topic>Neuropharmacology</topic><topic>Pain - physiopathology</topic><topic>Pharmacology. Drug treatments</topic><topic>Propylamines - pharmacology</topic><topic>Pyrroles - pharmacology</topic><topic>Pyrrolidines - pharmacology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Reflex - drug effects</topic><topic>Thiophenes - pharmacology</topic><topic>Visceral pain</topic><topic>κ-Opioid receptor</topic><topic>μ-Opioid receptor</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Langlois, Annik</creatorcontrib><creatorcontrib>Diop, Laurent</creatorcontrib><creatorcontrib>Rivière, Pierre J.M.</creatorcontrib><creatorcontrib>Pascaud, Xavier</creatorcontrib><creatorcontrib>Junien, Jean-Louis</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>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Langlois, Annik</au><au>Diop, Laurent</au><au>Rivière, Pierre J.M.</au><au>Pascaud, Xavier</au><au>Junien, Jean-Louis</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anesthetized rat</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1994-12-27</date><risdate>1994</risdate><volume>271</volume><issue>2</issue><spage>245</spage><epage>251</epage><pages>245-251</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The effect of fedotozine was evaluated in a model of colonic hypersensibility to balloon distension in anesthetized rats. Acetic acid (0.6%, intracolonically) significantly enhanced the hypotension reflex response to colonic distension (
P<0.05). At a noxious pain pressure (75 mm Hg), fedotozine ((+)-(−1
R)-1-phenyl-1-[(3,4,5-trimethoxy)benzyloxymethyl]-
N,
N-dimethyl-
n-propylamine) had no effect at 0.6 and 1 mg/kg i.v. in saline-treated rats and higher doses were required to produce antinociception (ED
50 = 2.57 mg/kg i.v.). By contrast, fedotozine at 0.6 and 1 mg/kg i.v. displayed 38 and 54% antinociception (
P < 0.05) respectively, in acetic acid-treated animals, leading to a decrease in its ED
50 (1.15 mg/kg i.v.). Similar results were obtained with (±)-
trans-
N-methyl-
N-[2-(pyrrolidinyl)-cyclohexyl]benzo[
b]-thiophene-4-acetamide (PD-117,302), a κ-opioid receptor agonist, while the antinociceptive action of morphine and a κ-opioid receptor agonist,
trans-(±)-3,4-dichloro-
N-methyl-
N-(2-[1-pyrrolidinyl] cyclohexyl)benzenacetamide ((±)-U-50,488H), was identical in control and acetic-treated animals. Nor-binaltorphimine, a selective κ-opioid receptor antagonist, reversed the enhanced antinociceptive activity of fedotozine and PD-117,302. It is concluded that acetic acid induces colonic hypersensibility to painful mechanical stimuli and that some but not all κ-opioid receptor ligands can have enhanced efficacy in this pathological situation.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>7705424</pmid><doi>10.1016/0014-2999(94)90780-3</doi><tpages>7</tpages></addata></record> |
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| ispartof | European journal of pharmacology, 1994-12, Vol.271 (2), p.245-251 |
| issn | 0014-2999 1879-0712 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_77799336 |
| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer Acetates Acetic Acid Amino Acid Sequence Analgesics Anesthesia Animals Benzyl Compounds - pharmacology Biological and medical sciences Blood Pressure - drug effects Colon - drug effects Colon - physiology Colonic hypersensitivity Dose-Response Relationship, Drug Fedotozine Male Medical sciences Molecular Sequence Data Neuropharmacology Pain - physiopathology Pharmacology. Drug treatments Propylamines - pharmacology Pyrroles - pharmacology Pyrrolidines - pharmacology Rats Rats, Sprague-Dawley Reflex - drug effects Thiophenes - pharmacology Visceral pain κ-Opioid receptor μ-Opioid receptor |
| title | Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anesthetized rat |
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