Effects of R56865 on membrane currents in isolated ventricular cardiomyocytes of the guinea-pig
In isolated heart muscle, the compound R56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine) has been shown to protect against intoxication by cardiac glycosides. We studied the influence of R56865 on various membrane currents in single isolated ventricular cardiomyocy...
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| Veröffentlicht in: | European journal of pharmacology 1990-10, Vol.187 (2), p.235-240 |
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| creator | Himmel, Herbert M. Wilhelm, Doris Ravens, Ursula |
| description | In isolated heart muscle, the compound R56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine) has been shown to protect against intoxication by cardiac glycosides. We studied the influence of R56865 on various membrane currents in single isolated ventricular cardiomyocytes of the guinea-pig. The sodium current, I
Na, was investigated at reduced extracellular Na
+ (30 mM) in the presence of Cd
2+ to block the calcium current, I
Ca, and with Cs
+ substituted for K
+ to reduce the K
+ currents, I
K. Under these conditions, R56865 concentration dependently decreased the peak I
Na with a half-maximum effect at about 1 μM. The steady state inactivation and normalized conductance of I
Na were not significantly different from the control. In ‘normal’ Tyrode solution, R56865 (10 μM) did not markedly reduce I
Ca, and did not affect the quasi steady state I
K, which was taken as an index of K
+ conductance. We conclude that R56865 possesses Na
+ channel-blocking properties, whereas I
Ca and membrane K
+ conductance were not influenced. |
| doi_str_mv | 10.1016/0014-2999(90)90010-4 |
| format | Article |
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Na, was investigated at reduced extracellular Na
+ (30 mM) in the presence of Cd
2+ to block the calcium current, I
Ca, and with Cs
+ substituted for K
+ to reduce the K
+ currents, I
K. Under these conditions, R56865 concentration dependently decreased the peak I
Na with a half-maximum effect at about 1 μM. The steady state inactivation and normalized conductance of I
Na were not significantly different from the control. In ‘normal’ Tyrode solution, R56865 (10 μM) did not markedly reduce I
Ca, and did not affect the quasi steady state I
K, which was taken as an index of K
+ conductance. We conclude that R56865 possesses Na
+ channel-blocking properties, whereas I
Ca and membrane K
+ conductance were not influenced.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(90)90010-4</identifier><identifier>PMID: 1703080</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Animals ; Benzothiazoles ; Biological and medical sciences ; Cadmium - pharmacology ; Cardiac glycoside intoxication ; Cardiomyocytes (isolated) ; Cardiovascular system ; Cesium - pharmacology ; Guinea Pigs ; Heart - drug effects ; In Vitro Techniques ; Ion Channels - drug effects ; Medical sciences ; Membrane currents ; Membranes - drug effects ; Membranes - metabolism ; Miscellaneous ; Myocardium - cytology ; Myocardium - metabolism ; Pharmacology. Drug treatments ; Piperidines - pharmacology ; Potassium Channels - drug effects ; R 56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine) ; Sodium Channels - drug effects ; Thiazoles - pharmacology</subject><ispartof>European journal of pharmacology, 1990-10, Vol.187 (2), p.235-240</ispartof><rights>1990</rights><rights>1991 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c418t-2074b1f34fac7343d9508b8447d5ee038dd5aad8694dd7ebd664701df267ee753</citedby><cites>FETCH-LOGICAL-c418t-2074b1f34fac7343d9508b8447d5ee038dd5aad8694dd7ebd664701df267ee753</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(90)90010-4$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=19336402$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1703080$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Himmel, Herbert M.</creatorcontrib><creatorcontrib>Wilhelm, Doris</creatorcontrib><creatorcontrib>Ravens, Ursula</creatorcontrib><title>Effects of R56865 on membrane currents in isolated ventricular cardiomyocytes of the guinea-pig</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>In isolated heart muscle, the compound R56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine) has been shown to protect against intoxication by cardiac glycosides. We studied the influence of R56865 on various membrane currents in single isolated ventricular cardiomyocytes of the guinea-pig. The sodium current, I
Na, was investigated at reduced extracellular Na
+ (30 mM) in the presence of Cd
2+ to block the calcium current, I
Ca, and with Cs
+ substituted for K
+ to reduce the K
+ currents, I
K. Under these conditions, R56865 concentration dependently decreased the peak I
Na with a half-maximum effect at about 1 μM. The steady state inactivation and normalized conductance of I
Na were not significantly different from the control. In ‘normal’ Tyrode solution, R56865 (10 μM) did not markedly reduce I
Ca, and did not affect the quasi steady state I
K, which was taken as an index of K
+ conductance. We conclude that R56865 possesses Na
+ channel-blocking properties, whereas I
Ca and membrane K
+ conductance were not influenced.</description><subject>Animals</subject><subject>Benzothiazoles</subject><subject>Biological and medical sciences</subject><subject>Cadmium - pharmacology</subject><subject>Cardiac glycoside intoxication</subject><subject>Cardiomyocytes (isolated)</subject><subject>Cardiovascular system</subject><subject>Cesium - pharmacology</subject><subject>Guinea Pigs</subject><subject>Heart - drug effects</subject><subject>In Vitro Techniques</subject><subject>Ion Channels - drug effects</subject><subject>Medical sciences</subject><subject>Membrane currents</subject><subject>Membranes - drug effects</subject><subject>Membranes - metabolism</subject><subject>Miscellaneous</subject><subject>Myocardium - cytology</subject><subject>Myocardium - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperidines - pharmacology</subject><subject>Potassium Channels - drug effects</subject><subject>R 56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine)</subject><subject>Sodium Channels - drug effects</subject><subject>Thiazoles - pharmacology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkUFrFTEUhYMo9Vn9BwrZWHQx9WaSTJKNIKWtQkEoug6Z5E6NzEyeyUzh_fvm9T3sTlchOd893JxDyFsG5wxY9wmAiaY1xnww8NHUGzTiGdkwrUwDirXPyeYv8pK8KuU3AEjTyhNywhRw0LAh9nIY0C-FpoHeyk53kqaZTjj12c1I_ZozzlWOM40ljW7BQO_rS45-HV2m3uUQ07RLfrfgo8vyC-ndGmd0zTbevSYvBjcWfHM8T8nPq8sfF1-bm-_X3y6-3DReML00LSjRs4GLwXnFBQ9Ggu61ECpIROA6BOlc0J0RISjsQ9cJBSwMbacQleSn5Ozgu83pz4plsVMsHsex_iKtxWpoGWtV91-QSW2U4ntQHECfUykZB7vNcXJ5ZxnYfQF2n67dp2sN2McCrKhj747-az9heBo6JF7190fdFe_GocbsY3nCDOedgLZynw8c1tTuI2ZbfMTZY4i5FmZDiv9e5AHr4aDw</recordid><startdate>19901009</startdate><enddate>19901009</enddate><creator>Himmel, Herbert M.</creator><creator>Wilhelm, Doris</creator><creator>Ravens, Ursula</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>8FD</scope><scope>FR3</scope><scope>M7Z</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>19901009</creationdate><title>Effects of R56865 on membrane currents in isolated ventricular cardiomyocytes of the guinea-pig</title><author>Himmel, Herbert M. ; Wilhelm, Doris ; Ravens, Ursula</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c418t-2074b1f34fac7343d9508b8447d5ee038dd5aad8694dd7ebd664701df267ee753</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>Animals</topic><topic>Benzothiazoles</topic><topic>Biological and medical sciences</topic><topic>Cadmium - pharmacology</topic><topic>Cardiac glycoside intoxication</topic><topic>Cardiomyocytes (isolated)</topic><topic>Cardiovascular system</topic><topic>Cesium - pharmacology</topic><topic>Guinea Pigs</topic><topic>Heart - drug effects</topic><topic>In Vitro Techniques</topic><topic>Ion Channels - drug effects</topic><topic>Medical sciences</topic><topic>Membrane currents</topic><topic>Membranes - drug effects</topic><topic>Membranes - metabolism</topic><topic>Miscellaneous</topic><topic>Myocardium - cytology</topic><topic>Myocardium - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperidines - pharmacology</topic><topic>Potassium Channels - drug effects</topic><topic>R 56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine)</topic><topic>Sodium Channels - drug effects</topic><topic>Thiazoles - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Himmel, Herbert M.</creatorcontrib><creatorcontrib>Wilhelm, Doris</creatorcontrib><creatorcontrib>Ravens, Ursula</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>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biochemistry Abstracts 1</collection><collection>Biotechnology and BioEngineering 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>Himmel, Herbert M.</au><au>Wilhelm, Doris</au><au>Ravens, Ursula</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effects of R56865 on membrane currents in isolated ventricular cardiomyocytes of the guinea-pig</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1990-10-09</date><risdate>1990</risdate><volume>187</volume><issue>2</issue><spage>235</spage><epage>240</epage><pages>235-240</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>In isolated heart muscle, the compound R56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine) has been shown to protect against intoxication by cardiac glycosides. We studied the influence of R56865 on various membrane currents in single isolated ventricular cardiomyocytes of the guinea-pig. The sodium current, I
Na, was investigated at reduced extracellular Na
+ (30 mM) in the presence of Cd
2+ to block the calcium current, I
Ca, and with Cs
+ substituted for K
+ to reduce the K
+ currents, I
K. Under these conditions, R56865 concentration dependently decreased the peak I
Na with a half-maximum effect at about 1 μM. The steady state inactivation and normalized conductance of I
Na were not significantly different from the control. In ‘normal’ Tyrode solution, R56865 (10 μM) did not markedly reduce I
Ca, and did not affect the quasi steady state I
K, which was taken as an index of K
+ conductance. We conclude that R56865 possesses Na
+ channel-blocking properties, whereas I
Ca and membrane K
+ conductance were not influenced.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>1703080</pmid><doi>10.1016/0014-2999(90)90010-4</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
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| issn | 0014-2999 1879-0712 |
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| subjects | Animals Benzothiazoles Biological and medical sciences Cadmium - pharmacology Cardiac glycoside intoxication Cardiomyocytes (isolated) Cardiovascular system Cesium - pharmacology Guinea Pigs Heart - drug effects In Vitro Techniques Ion Channels - drug effects Medical sciences Membrane currents Membranes - drug effects Membranes - metabolism Miscellaneous Myocardium - cytology Myocardium - metabolism Pharmacology. Drug treatments Piperidines - pharmacology Potassium Channels - drug effects R 56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine) Sodium Channels - drug effects Thiazoles - pharmacology |
| title | Effects of R56865 on membrane currents in isolated ventricular cardiomyocytes of the guinea-pig |
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