Analysis of the mechanism underlying the peripheral antinociceptive action of sildenafil in the formalin test
The mechanism of the antinociceptive action of the phosphodiesterase 5 inhibitor, sildenafil, was assessed in the formalin test. Local peripheral ipsilateral, but not contralateral, administration of sildenafil (50–200 μg/paw) produced a dose-related antinociception during both phases of the formali...
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| Veröffentlicht in: | European journal of pharmacology 2005-04, Vol.512 (2), p.121-127 |
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| container_title | European journal of pharmacology |
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| creator | Ambriz-Tututi, Mónica Velázquez-Zamora, Dulce A. Urquiza-Marín, Héctor Granados-Soto, Vinicio |
| description | The mechanism of the antinociceptive action of the phosphodiesterase 5 inhibitor, sildenafil, was assessed in the formalin test. Local peripheral ipsilateral, but not contralateral, administration of sildenafil (50–200 μg/paw) produced a dose-related antinociception during both phases of the formalin test. The local peripheral pretreatment with protein kinase G inhibitor peptide (PKG inhibitor, 0.01–1 μg/paw), charybdotoxin (large- and intermediate-conductance Ca
2
+-activated K
+ channel blocker, 0.01–1 μg/paw), apamin (small-conductance Ca
2
+-activated K
+ channel blocker, 0.1–2 μg/paw), tolbutamide (ATP-sensitive K
+ channel blocker, 12.5–50 μg/paw), and tetraethylammonium (non-selective voltage-dependent K
+ channel blocker, 12.5–50 μg/paw), but not 1
H-(1,2,4)-oxadiazolo(4,2-
a)quinoxalin-1-one (ODQ, inhibitor of guanylyl cyclase, 12.5–50 μg/paw) or saline, significantly diminished in a dose-dependent manner sildenafil-induced local peripheral antinociception. Given alone, local peripheral administration of inhibitors did not modify formalin-induced nociceptive behavior. Results suggest that sildenafil produces its local peripheral antinociceptive effect via activation of the cyclic GMP–PKG–K
+ channel pathway. |
| doi_str_mv | 10.1016/j.ejphar.2005.01.055 |
| format | Article |
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2
+-activated K
+ channel blocker, 0.01–1 μg/paw), apamin (small-conductance Ca
2
+-activated K
+ channel blocker, 0.1–2 μg/paw), tolbutamide (ATP-sensitive K
+ channel blocker, 12.5–50 μg/paw), and tetraethylammonium (non-selective voltage-dependent K
+ channel blocker, 12.5–50 μg/paw), but not 1
H-(1,2,4)-oxadiazolo(4,2-
a)quinoxalin-1-one (ODQ, inhibitor of guanylyl cyclase, 12.5–50 μg/paw) or saline, significantly diminished in a dose-dependent manner sildenafil-induced local peripheral antinociception. Given alone, local peripheral administration of inhibitors did not modify formalin-induced nociceptive behavior. Results suggest that sildenafil produces its local peripheral antinociceptive effect via activation of the cyclic GMP–PKG–K
+ channel pathway.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/j.ejphar.2005.01.055</identifier><identifier>PMID: 15840396</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Analgesics - pharmacology ; Animals ; Apamin - pharmacology ; Biological and medical sciences ; Charybdotoxin - pharmacology ; Cyclic GMP ; Cyclic GMP-Dependent Protein Kinases - antagonists & inhibitors ; Dose-Response Relationship, Drug ; Enzyme Inhibitors - pharmacology ; Female ; Formaldehyde ; Guanylate Cyclase - antagonists & inhibitors ; Injections, Subcutaneous ; K + channel ; Medical sciences ; Oxadiazoles - pharmacology ; Pain - chemically induced ; Pain - prevention & control ; Pain Measurement - methods ; Peripheral processing ; Pharmacology. Drug treatments ; Piperazines - pharmacology ; Potassium Channel Blockers - pharmacology ; Protein kinase G ; Purines ; Quinoxalines - pharmacology ; Rats ; Rats, Wistar ; Sildenafil ; Sildenafil Citrate ; Sulfones ; Tetraethylammonium - pharmacology ; Time Factors ; Tolbutamide - pharmacology</subject><ispartof>European journal of pharmacology, 2005-04, Vol.512 (2), p.121-127</ispartof><rights>2005 Elsevier B.V.</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c421t-eaa36bd4cfd5e3cf0afe4b47b1f48d6b4c7c33db1b46598f66fae926914d7cbc3</citedby><cites>FETCH-LOGICAL-c421t-eaa36bd4cfd5e3cf0afe4b47b1f48d6b4c7c33db1b46598f66fae926914d7cbc3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ejphar.2005.01.055$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16713826$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15840396$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ambriz-Tututi, Mónica</creatorcontrib><creatorcontrib>Velázquez-Zamora, Dulce A.</creatorcontrib><creatorcontrib>Urquiza-Marín, Héctor</creatorcontrib><creatorcontrib>Granados-Soto, Vinicio</creatorcontrib><title>Analysis of the mechanism underlying the peripheral antinociceptive action of sildenafil in the formalin test</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>The mechanism of the antinociceptive action of the phosphodiesterase 5 inhibitor, sildenafil, was assessed in the formalin test. Local peripheral ipsilateral, but not contralateral, administration of sildenafil (50–200 μg/paw) produced a dose-related antinociception during both phases of the formalin test. The local peripheral pretreatment with protein kinase G inhibitor peptide (PKG inhibitor, 0.01–1 μg/paw), charybdotoxin (large- and intermediate-conductance Ca
2
+-activated K
+ channel blocker, 0.01–1 μg/paw), apamin (small-conductance Ca
2
+-activated K
+ channel blocker, 0.1–2 μg/paw), tolbutamide (ATP-sensitive K
+ channel blocker, 12.5–50 μg/paw), and tetraethylammonium (non-selective voltage-dependent K
+ channel blocker, 12.5–50 μg/paw), but not 1
H-(1,2,4)-oxadiazolo(4,2-
a)quinoxalin-1-one (ODQ, inhibitor of guanylyl cyclase, 12.5–50 μg/paw) or saline, significantly diminished in a dose-dependent manner sildenafil-induced local peripheral antinociception. Given alone, local peripheral administration of inhibitors did not modify formalin-induced nociceptive behavior. Results suggest that sildenafil produces its local peripheral antinociceptive effect via activation of the cyclic GMP–PKG–K
+ channel pathway.</description><subject>Analgesics - pharmacology</subject><subject>Animals</subject><subject>Apamin - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Charybdotoxin - pharmacology</subject><subject>Cyclic GMP</subject><subject>Cyclic GMP-Dependent Protein Kinases - antagonists & inhibitors</subject><subject>Dose-Response Relationship, Drug</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Female</subject><subject>Formaldehyde</subject><subject>Guanylate Cyclase - antagonists & inhibitors</subject><subject>Injections, Subcutaneous</subject><subject>K + channel</subject><subject>Medical sciences</subject><subject>Oxadiazoles - pharmacology</subject><subject>Pain - chemically induced</subject><subject>Pain - prevention & control</subject><subject>Pain Measurement - methods</subject><subject>Peripheral processing</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperazines - pharmacology</subject><subject>Potassium Channel Blockers - pharmacology</subject><subject>Protein kinase G</subject><subject>Purines</subject><subject>Quinoxalines - pharmacology</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Sildenafil</subject><subject>Sildenafil Citrate</subject><subject>Sulfones</subject><subject>Tetraethylammonium - pharmacology</subject><subject>Time Factors</subject><subject>Tolbutamide - pharmacology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMFu1DAQhi0EotvCGyCUC9wS7MRx4gtSVQFFqsQFzpYzHrOzcpxgZyvt2zfprtQbJ2vk7_9n9DH2QfBKcKG-HCo8zHubqprztuKi4m37iu1E3-mSd6J-zXacC1nWWusrdp3zga-grtu37Eq0veSNVjs23kYbTplyMfli2WMxIuxtpDwWx-gwhRPFv88fMyaa95hsKGxcKE5AgPNCj1hYWGiKW0Om4DBaT6Gg-BzzUxpt2AbMyzv2xtuQ8f3lvWF_vn_7fXdfPvz68fPu9qEEWYulRGsbNTgJ3rXYgOfWoxxkNwgve6cGCR00jRvEIFWre6-Ut6hrpYV0HQzQ3LDP5945Tf-O62IzUgYMwUacjtmIrlEt7_gKyjMIaco5oTdzotGmkxHcbJrNwZw1m02z4cKsmtfYx0v_cRjRvYQuXlfg0wWwGWzwyUag_MKpTjR9vXFfzxyuNh4Jk8lAGAEdJYTFuIn-f8kTFv2geA</recordid><startdate>20050411</startdate><enddate>20050411</enddate><creator>Ambriz-Tututi, Mónica</creator><creator>Velázquez-Zamora, Dulce A.</creator><creator>Urquiza-Marín, Héctor</creator><creator>Granados-Soto, Vinicio</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></search><sort><creationdate>20050411</creationdate><title>Analysis of the mechanism underlying the peripheral antinociceptive action of sildenafil in the formalin test</title><author>Ambriz-Tututi, Mónica ; Velázquez-Zamora, Dulce A. ; Urquiza-Marín, Héctor ; Granados-Soto, Vinicio</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c421t-eaa36bd4cfd5e3cf0afe4b47b1f48d6b4c7c33db1b46598f66fae926914d7cbc3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Analgesics - pharmacology</topic><topic>Animals</topic><topic>Apamin - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Charybdotoxin - pharmacology</topic><topic>Cyclic GMP</topic><topic>Cyclic GMP-Dependent Protein Kinases - antagonists & inhibitors</topic><topic>Dose-Response Relationship, Drug</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Female</topic><topic>Formaldehyde</topic><topic>Guanylate Cyclase - antagonists & inhibitors</topic><topic>Injections, Subcutaneous</topic><topic>K + channel</topic><topic>Medical sciences</topic><topic>Oxadiazoles - pharmacology</topic><topic>Pain - chemically induced</topic><topic>Pain - prevention & control</topic><topic>Pain Measurement - methods</topic><topic>Peripheral processing</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperazines - pharmacology</topic><topic>Potassium Channel Blockers - pharmacology</topic><topic>Protein kinase G</topic><topic>Purines</topic><topic>Quinoxalines - pharmacology</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Sildenafil</topic><topic>Sildenafil Citrate</topic><topic>Sulfones</topic><topic>Tetraethylammonium - pharmacology</topic><topic>Time Factors</topic><topic>Tolbutamide - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ambriz-Tututi, Mónica</creatorcontrib><creatorcontrib>Velázquez-Zamora, Dulce A.</creatorcontrib><creatorcontrib>Urquiza-Marín, Héctor</creatorcontrib><creatorcontrib>Granados-Soto, Vinicio</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><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ambriz-Tututi, Mónica</au><au>Velázquez-Zamora, Dulce A.</au><au>Urquiza-Marín, Héctor</au><au>Granados-Soto, Vinicio</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Analysis of the mechanism underlying the peripheral antinociceptive action of sildenafil in the formalin test</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>2005-04-11</date><risdate>2005</risdate><volume>512</volume><issue>2</issue><spage>121</spage><epage>127</epage><pages>121-127</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The mechanism of the antinociceptive action of the phosphodiesterase 5 inhibitor, sildenafil, was assessed in the formalin test. Local peripheral ipsilateral, but not contralateral, administration of sildenafil (50–200 μg/paw) produced a dose-related antinociception during both phases of the formalin test. The local peripheral pretreatment with protein kinase G inhibitor peptide (PKG inhibitor, 0.01–1 μg/paw), charybdotoxin (large- and intermediate-conductance Ca
2
+-activated K
+ channel blocker, 0.01–1 μg/paw), apamin (small-conductance Ca
2
+-activated K
+ channel blocker, 0.1–2 μg/paw), tolbutamide (ATP-sensitive K
+ channel blocker, 12.5–50 μg/paw), and tetraethylammonium (non-selective voltage-dependent K
+ channel blocker, 12.5–50 μg/paw), but not 1
H-(1,2,4)-oxadiazolo(4,2-
a)quinoxalin-1-one (ODQ, inhibitor of guanylyl cyclase, 12.5–50 μg/paw) or saline, significantly diminished in a dose-dependent manner sildenafil-induced local peripheral antinociception. Given alone, local peripheral administration of inhibitors did not modify formalin-induced nociceptive behavior. Results suggest that sildenafil produces its local peripheral antinociceptive effect via activation of the cyclic GMP–PKG–K
+ channel pathway.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>15840396</pmid><doi>10.1016/j.ejphar.2005.01.055</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | European journal of pharmacology, 2005-04, Vol.512 (2), p.121-127 |
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| language | eng |
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| subjects | Analgesics - pharmacology Animals Apamin - pharmacology Biological and medical sciences Charybdotoxin - pharmacology Cyclic GMP Cyclic GMP-Dependent Protein Kinases - antagonists & inhibitors Dose-Response Relationship, Drug Enzyme Inhibitors - pharmacology Female Formaldehyde Guanylate Cyclase - antagonists & inhibitors Injections, Subcutaneous K + channel Medical sciences Oxadiazoles - pharmacology Pain - chemically induced Pain - prevention & control Pain Measurement - methods Peripheral processing Pharmacology. Drug treatments Piperazines - pharmacology Potassium Channel Blockers - pharmacology Protein kinase G Purines Quinoxalines - pharmacology Rats Rats, Wistar Sildenafil Sildenafil Citrate Sulfones Tetraethylammonium - pharmacology Time Factors Tolbutamide - pharmacology |
| title | Analysis of the mechanism underlying the peripheral antinociceptive action of sildenafil in the formalin test |
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