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Electrophysiological effects of diclofurime on rabbit and frog atrial heart muscle
1 The effects of diclofurime on the electrical activity of the rabbit sinus node, rabbit atria and frog atrial fibres were studied using microelectrode and the double sucrose gap voltage‐clamp techniques respectively. 2 In rabbit sinus node, diclofurime (10−7 m to 10−6 m) decreased the action potent...
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| Published in: | British journal of pharmacology 1987-04, Vol.90 (4), p.717-725 |
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| Language: | English |
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| cites | cdi_FETCH-LOGICAL-c5075-558c112233b635b8fcc3ff23e5eaf63911a23b950f396120f7894efeac78e82d3 |
| container_end_page | 725 |
| container_issue | 4 |
| container_start_page | 717 |
| container_title | British journal of pharmacology |
| container_volume | 90 |
| creator | Gautier, Patrick Guiraudou, Pierre Sauviat, Martin‐Pierre |
| description | 1
The effects of diclofurime on the electrical activity of the rabbit sinus node, rabbit atria and frog atrial fibres were studied using microelectrode and the double sucrose gap voltage‐clamp techniques respectively.
2
In rabbit sinus node, diclofurime (10−7 m to 10−6 m) decreased the action potential (AP) amplitude and maximum rate of depolarization , increased the AP duration and slowed the sinus rate.
3
In rabbit atria, the drug reduced the amplitude of the depolarizing phase and , lengthened the AP duration and decreased the resting membrane potential.
4
In frog atrial fibres, the drug (10−5 m) depolarized the resting membrane potential, decreased as well as the plateau amplitude. It inhibited the sodium current (INa) with a dissociation constant of 3.7 × 10−6 M and a one to one relationship between the drug molecule and the Na channel. Diclofurime did not alter the apparent reversal potential for the fast Na current (ENa) but it inhibited the sodium conductance (GNa) in a frequency‐dependent manner.
5
Diclofurime also blocked the slow inward current (Islow) without alteration of Eslow. The block of Islow occurred with a dissociation constant of 2 × 10−5 m and unity stoichiometry.
6
The data suggest that diclofurime might be effective in the control of cardiac arrythmias since it exhibited both local anaesthetic‐like and calcium antagonistic properties. |
| doi_str_mv | 10.1111/j.1476-5381.1987.tb11225.x |
| format | article |
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The effects of diclofurime on the electrical activity of the rabbit sinus node, rabbit atria and frog atrial fibres were studied using microelectrode and the double sucrose gap voltage‐clamp techniques respectively.
2
In rabbit sinus node, diclofurime (10−7 m to 10−6 m) decreased the action potential (AP) amplitude and maximum rate of depolarization , increased the AP duration and slowed the sinus rate.
3
In rabbit atria, the drug reduced the amplitude of the depolarizing phase and , lengthened the AP duration and decreased the resting membrane potential.
4
In frog atrial fibres, the drug (10−5 m) depolarized the resting membrane potential, decreased as well as the plateau amplitude. It inhibited the sodium current (INa) with a dissociation constant of 3.7 × 10−6 M and a one to one relationship between the drug molecule and the Na channel. Diclofurime did not alter the apparent reversal potential for the fast Na current (ENa) but it inhibited the sodium conductance (GNa) in a frequency‐dependent manner.
5
Diclofurime also blocked the slow inward current (Islow) without alteration of Eslow. The block of Islow occurred with a dissociation constant of 2 × 10−5 m and unity stoichiometry.
6
The data suggest that diclofurime might be effective in the control of cardiac arrythmias since it exhibited both local anaesthetic‐like and calcium antagonistic properties.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1987.tb11225.x</identifier><identifier>PMID: 3580705</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Action Potentials - drug effects ; Animals ; Biological and medical sciences ; Cardiovascular system ; Dose-Response Relationship, Drug ; Female ; Heart - drug effects ; Heart - physiology ; In Vitro Techniques ; Male ; Medical sciences ; Oximes - pharmacology ; Pharmacology. Drug treatments ; Rabbits ; Sodium - metabolism ; Vasodilator Agents - pharmacology ; Vasodilator agents. Cerebral vasodilators</subject><ispartof>British journal of pharmacology, 1987-04, Vol.90 (4), p.717-725</ispartof><rights>1987 British Pharmacological Society</rights><rights>1988 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5075-558c112233b635b8fcc3ff23e5eaf63911a23b950f396120f7894efeac78e82d3</citedby><cites>FETCH-LOGICAL-c5075-558c112233b635b8fcc3ff23e5eaf63911a23b950f396120f7894efeac78e82d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917206/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917206/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,315,733,786,790,891,1424,27957,27958,45609,45610,53827,53829</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7495829$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3580705$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Gautier, Patrick</creatorcontrib><creatorcontrib>Guiraudou, Pierre</creatorcontrib><creatorcontrib>Sauviat, Martin‐Pierre</creatorcontrib><title>Electrophysiological effects of diclofurime on rabbit and frog atrial heart muscle</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
The effects of diclofurime on the electrical activity of the rabbit sinus node, rabbit atria and frog atrial fibres were studied using microelectrode and the double sucrose gap voltage‐clamp techniques respectively.
2
In rabbit sinus node, diclofurime (10−7 m to 10−6 m) decreased the action potential (AP) amplitude and maximum rate of depolarization , increased the AP duration and slowed the sinus rate.
3
In rabbit atria, the drug reduced the amplitude of the depolarizing phase and , lengthened the AP duration and decreased the resting membrane potential.
4
In frog atrial fibres, the drug (10−5 m) depolarized the resting membrane potential, decreased as well as the plateau amplitude. It inhibited the sodium current (INa) with a dissociation constant of 3.7 × 10−6 M and a one to one relationship between the drug molecule and the Na channel. Diclofurime did not alter the apparent reversal potential for the fast Na current (ENa) but it inhibited the sodium conductance (GNa) in a frequency‐dependent manner.
5
Diclofurime also blocked the slow inward current (Islow) without alteration of Eslow. The block of Islow occurred with a dissociation constant of 2 × 10−5 m and unity stoichiometry.
6
The data suggest that diclofurime might be effective in the control of cardiac arrythmias since it exhibited both local anaesthetic‐like and calcium antagonistic properties.</description><subject>Action Potentials - drug effects</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cardiovascular system</subject><subject>Dose-Response Relationship, Drug</subject><subject>Female</subject><subject>Heart - drug effects</subject><subject>Heart - physiology</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Oximes - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Rabbits</subject><subject>Sodium - metabolism</subject><subject>Vasodilator Agents - pharmacology</subject><subject>Vasodilator agents. Cerebral vasodilators</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><recordid>eNqVUU1vEzEUtBBVCYWfgGQhxG23_ojXXg6oUBWKVAmE4Gx5nefEkbMO9i40_x4vWUXlWF9seebNG80g9JqSmpZzua3pUjaV4IrWtFWyHjpKGRP1_RO0OEFP0YIQIitKlXqGnue8JaSAUpyjcy4UkUQs0PebAHZIcb85ZB9DXHtrAgbnym_G0eGVtyG6Mfkd4NjjZLrOD9j0K-xSXGMzJF8GNmDSgHdjtgFeoDNnQoaX832Bfn66-XF9W919_fzl-sNdZQWRohJC2ck1513DRaectdw5xkGAcQ1vKTWMd60gjrcNZcRJ1S7BgbFSgWIrfoHeH3X3Y7eDlYV-SCbofbFq0kFH4_X_SO83eh1_a9pSyUhTBN7OAin-GiEPeuezhRBMD3HMukTFOVOyEN8diTbFnBO40xJK9NSI3uopdj3FrqdG9NyIvi_Drx7aPI3OFRT8zYybXLJ3yfTW5xNNLluhWFtoV0faHx_g8AgD-uO3239P_hclHaqD</recordid><startdate>198704</startdate><enddate>198704</enddate><creator>Gautier, Patrick</creator><creator>Guiraudou, Pierre</creator><creator>Sauviat, Martin‐Pierre</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</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><scope>5PM</scope></search><sort><creationdate>198704</creationdate><title>Electrophysiological effects of diclofurime on rabbit and frog atrial heart muscle</title><author>Gautier, Patrick ; Guiraudou, Pierre ; Sauviat, Martin‐Pierre</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5075-558c112233b635b8fcc3ff23e5eaf63911a23b950f396120f7894efeac78e82d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Action Potentials - drug effects</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cardiovascular system</topic><topic>Dose-Response Relationship, Drug</topic><topic>Female</topic><topic>Heart - drug effects</topic><topic>Heart - physiology</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Oximes - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Rabbits</topic><topic>Sodium - metabolism</topic><topic>Vasodilator Agents - pharmacology</topic><topic>Vasodilator agents. Cerebral vasodilators</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Gautier, Patrick</creatorcontrib><creatorcontrib>Guiraudou, Pierre</creatorcontrib><creatorcontrib>Sauviat, Martin‐Pierre</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><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Gautier, Patrick</au><au>Guiraudou, Pierre</au><au>Sauviat, Martin‐Pierre</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Electrophysiological effects of diclofurime on rabbit and frog atrial heart muscle</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1987-04</date><risdate>1987</risdate><volume>90</volume><issue>4</issue><spage>717</spage><epage>725</epage><pages>717-725</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><notes>ObjectType-Article-1</notes><notes>SourceType-Scholarly Journals-1</notes><notes>ObjectType-Feature-2</notes><notes>content type line 23</notes><abstract>1
The effects of diclofurime on the electrical activity of the rabbit sinus node, rabbit atria and frog atrial fibres were studied using microelectrode and the double sucrose gap voltage‐clamp techniques respectively.
2
In rabbit sinus node, diclofurime (10−7 m to 10−6 m) decreased the action potential (AP) amplitude and maximum rate of depolarization , increased the AP duration and slowed the sinus rate.
3
In rabbit atria, the drug reduced the amplitude of the depolarizing phase and , lengthened the AP duration and decreased the resting membrane potential.
4
In frog atrial fibres, the drug (10−5 m) depolarized the resting membrane potential, decreased as well as the plateau amplitude. It inhibited the sodium current (INa) with a dissociation constant of 3.7 × 10−6 M and a one to one relationship between the drug molecule and the Na channel. Diclofurime did not alter the apparent reversal potential for the fast Na current (ENa) but it inhibited the sodium conductance (GNa) in a frequency‐dependent manner.
5
Diclofurime also blocked the slow inward current (Islow) without alteration of Eslow. The block of Islow occurred with a dissociation constant of 2 × 10−5 m and unity stoichiometry.
6
The data suggest that diclofurime might be effective in the control of cardiac arrythmias since it exhibited both local anaesthetic‐like and calcium antagonistic properties.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>3580705</pmid><doi>10.1111/j.1476-5381.1987.tb11225.x</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0007-1188 |
| ispartof | British journal of pharmacology, 1987-04, Vol.90 (4), p.717-725 |
| issn | 0007-1188 1476-5381 |
| language | eng |
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| source | Wiley-Blackwell Journals; PubMed Central（OA） |
| subjects | Action Potentials - drug effects Animals Biological and medical sciences Cardiovascular system Dose-Response Relationship, Drug Female Heart - drug effects Heart - physiology In Vitro Techniques Male Medical sciences Oximes - pharmacology Pharmacology. Drug treatments Rabbits Sodium - metabolism Vasodilator Agents - pharmacology Vasodilator agents. Cerebral vasodilators |
| title | Electrophysiological effects of diclofurime on rabbit and frog atrial heart muscle |
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