NS 1619 activates BKCa channel activity in rat cortical neurones
Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-...
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| Veröffentlicht in: | European journal of pharmacology 1995-07, Vol.280 (2), p.215-219 |
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| container_title | European journal of pharmacology |
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| creator | LEE, K ROWE, I. C. M ASHFORD, M. L. J |
| description | Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation. |
| doi_str_mv | 10.1016/0014-2999(95)00251-F |
| format | Article |
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Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(95)00251-F</identifier><identifier>PMID: 7589189</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Adenosine Triphosphate - pharmacology ; Animals ; Benzimidazoles - pharmacology ; Biological and medical sciences ; Calcium - physiology ; In Vitro Techniques ; Male ; Medical sciences ; Miscellaneous ; Motor Cortex - cytology ; Motor Cortex - drug effects ; Motor Cortex - metabolism ; Neurons - drug effects ; Neurons - metabolism ; Neuropharmacology ; Pharmacology. 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C. M</creatorcontrib><creatorcontrib>ASHFORD, M. L. J</creatorcontrib><title>NS 1619 activates BKCa channel activity in rat cortical neurones</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation.</description><subject>Adenosine Triphosphate - pharmacology</subject><subject>Animals</subject><subject>Benzimidazoles - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Calcium - physiology</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Motor Cortex - cytology</subject><subject>Motor Cortex - drug effects</subject><subject>Motor Cortex - metabolism</subject><subject>Neurons - drug effects</subject><subject>Neurons - metabolism</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Potassium Channels - drug effects</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kM1OwzAQhC0EKqXwBiD5gBAcAuu_2r4BFQVEBQfgbDmOLYLSpNgJUt-elEY9rXZnZqX5EDolcE2ATG8ACM-o1vpSiysAKkg230NjoqTOQBK6j8Y7yyE6SukbAISmYoRGUihNlB6j29d3TKZEY-va8te2PuH7l5nF7svWta-257Jd47LG0bbYNbEtna1w7bvY1D4do4Ngq-RPhjlBn_OHj9lTtnh7fJ7dLTJHtWyzkAsrgfNArOJFzkPBPJPgCztVlvcSpTmRqghaBy8dQAGMhqBov3LnGJugi-3fVWx-Op9asyyT81Vla990yUg57atR6I18a3SxSSn6YFaxXNq4NgTMBpzZUDEbKkYL8w_OzPvY2fC_y5e-2IUGUr1-Pug29f1DtLUr087GhJKcSfYHUid0gg</recordid><startdate>19950704</startdate><enddate>19950704</enddate><creator>LEE, K</creator><creator>ROWE, I. C. M</creator><creator>ASHFORD, M. L. 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Drug treatments</topic><topic>Potassium Channels - drug effects</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>LEE, K</creatorcontrib><creatorcontrib>ROWE, I. C. M</creatorcontrib><creatorcontrib>ASHFORD, M. L. J</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>LEE, K</au><au>ROWE, I. C. M</au><au>ASHFORD, M. L. J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>NS 1619 activates BKCa channel activity in rat cortical neurones</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1995-07-04</date><risdate>1995</risdate><volume>280</volume><issue>2</issue><spage>215</spage><epage>219</epage><pages>215-219</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. 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| ispartof | European journal of pharmacology, 1995-07, Vol.280 (2), p.215-219 |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Adenosine Triphosphate - pharmacology Animals Benzimidazoles - pharmacology Biological and medical sciences Calcium - physiology In Vitro Techniques Male Medical sciences Miscellaneous Motor Cortex - cytology Motor Cortex - drug effects Motor Cortex - metabolism Neurons - drug effects Neurons - metabolism Neuropharmacology Pharmacology. Drug treatments Potassium Channels - drug effects Rats Rats, Sprague-Dawley |
| title | NS 1619 activates BKCa channel activity in rat cortical neurones |
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