The potassium channel opener BRL 38227 inhibits binding of [ 125I]-labelled endothelin-1 to rat cardiac membranes
Binding of [ 125I]-labelled endothelin-1 (ET-1) to rat cardiac membranes and the effects of endothelin-1 (ET-1), endothelin-3 (ET-3), the calcium channel antagonist nifedipine, and both enantiomers of the potassium channel opener cromakalim (BRL 34915) on binding have been examined. Specific binding...
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| Veröffentlicht in: | Biochemical and biophysical research communications 1992-06, Vol.185 (2), p.630-635 |
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| container_title | Biochemical and biophysical research communications |
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| creator | Waugh, Christopher J. Dockrell, Mark E.C. Haynes, William G. Olverman, Henry J. Williams, Brent C. Webb, David J. |
| description | Binding of [
125I]-labelled endothelin-1 (ET-1) to rat cardiac membranes and the effects of endothelin-1 (ET-1), endothelin-3 (ET-3), the calcium channel antagonist nifedipine, and both enantiomers of the potassium channel opener cromakalim (BRL 34915) on binding have been examined. Specific binding of [
125I]-ET-1 was inhibited in a concentration dependent manner by both unlabelled ET-1 (10
−12 – 10
−7 M) and ET-3 (10
−12 – 10
−6 M). Nifedipine (10
−11 – 10
−5 M) did not affect [
125I]-ET-1 binding. However, BRL 38227 (10
−11 – 10
−5 M), the biologically active isomer of cromakalim, significantly inhibited [
125I]-ET-1 binding. The inactive isomer, BRL 38226 (10
−11 – 10
−5 M) had no effect. These findings provide the first evidence for a stereospecific interaction between BRL 38227 and an ET-1 binding site in rat cardiac membranes. |
| doi_str_mv | 10.1016/0006-291X(92)91671-C |
| format | Article |
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125I]-labelled endothelin-1 (ET-1) to rat cardiac membranes and the effects of endothelin-1 (ET-1), endothelin-3 (ET-3), the calcium channel antagonist nifedipine, and both enantiomers of the potassium channel opener cromakalim (BRL 34915) on binding have been examined. Specific binding of [
125I]-ET-1 was inhibited in a concentration dependent manner by both unlabelled ET-1 (10
−12 – 10
−7 M) and ET-3 (10
−12 – 10
−6 M). Nifedipine (10
−11 – 10
−5 M) did not affect [
125I]-ET-1 binding. However, BRL 38227 (10
−11 – 10
−5 M), the biologically active isomer of cromakalim, significantly inhibited [
125I]-ET-1 binding. The inactive isomer, BRL 38226 (10
−11 – 10
−5 M) had no effect. These findings provide the first evidence for a stereospecific interaction between BRL 38227 and an ET-1 binding site in rat cardiac membranes.</description><identifier>ISSN: 0006-291X</identifier><identifier>EISSN: 1090-2104</identifier><identifier>DOI: 10.1016/0006-291X(92)91671-C</identifier><identifier>PMID: 1610355</identifier><identifier>CODEN: BBRCA9</identifier><language>eng</language><publisher>San Diego, CA: Elsevier Inc</publisher><subject>Animals ; Benzopyrans - metabolism ; Benzopyrans - pharmacology ; Binding, Competitive ; Biological and medical sciences ; Blood vessels and receptors ; Cromakalim ; Endothelins - metabolism ; Fundamental and applied biological sciences. Psychology ; In Vitro Techniques ; Ion Channel Gating - drug effects ; Myocardium - metabolism ; Nifedipine - pharmacology ; Potassium Channels - drug effects ; Pyrroles - metabolism ; Pyrroles - pharmacology ; Rats ; Sarcolemma - metabolism ; Vertebrates: cardiovascular system</subject><ispartof>Biochemical and biophysical research communications, 1992-06, Vol.185 (2), p.630-635</ispartof><rights>1992</rights><rights>1992 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-edda204911b0066ac1d13bde6c9563dda2840cb4a09212ada9401011b5717d6d3</citedby><cites>FETCH-LOGICAL-c386t-edda204911b0066ac1d13bde6c9563dda2840cb4a09212ada9401011b5717d6d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0006-291X(92)91671-C$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=5347850$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1610355$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Waugh, Christopher J.</creatorcontrib><creatorcontrib>Dockrell, Mark E.C.</creatorcontrib><creatorcontrib>Haynes, William G.</creatorcontrib><creatorcontrib>Olverman, Henry J.</creatorcontrib><creatorcontrib>Williams, Brent C.</creatorcontrib><creatorcontrib>Webb, David J.</creatorcontrib><title>The potassium channel opener BRL 38227 inhibits binding of [ 125I]-labelled endothelin-1 to rat cardiac membranes</title><title>Biochemical and biophysical research communications</title><addtitle>Biochem Biophys Res Commun</addtitle><description>Binding of [
125I]-labelled endothelin-1 (ET-1) to rat cardiac membranes and the effects of endothelin-1 (ET-1), endothelin-3 (ET-3), the calcium channel antagonist nifedipine, and both enantiomers of the potassium channel opener cromakalim (BRL 34915) on binding have been examined. Specific binding of [
125I]-ET-1 was inhibited in a concentration dependent manner by both unlabelled ET-1 (10
−12 – 10
−7 M) and ET-3 (10
−12 – 10
−6 M). Nifedipine (10
−11 – 10
−5 M) did not affect [
125I]-ET-1 binding. However, BRL 38227 (10
−11 – 10
−5 M), the biologically active isomer of cromakalim, significantly inhibited [
125I]-ET-1 binding. The inactive isomer, BRL 38226 (10
−11 – 10
−5 M) had no effect. These findings provide the first evidence for a stereospecific interaction between BRL 38227 and an ET-1 binding site in rat cardiac membranes.</description><subject>Animals</subject><subject>Benzopyrans - metabolism</subject><subject>Benzopyrans - pharmacology</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Blood vessels and receptors</subject><subject>Cromakalim</subject><subject>Endothelins - metabolism</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>In Vitro Techniques</subject><subject>Ion Channel Gating - drug effects</subject><subject>Myocardium - metabolism</subject><subject>Nifedipine - pharmacology</subject><subject>Potassium Channels - drug effects</subject><subject>Pyrroles - metabolism</subject><subject>Pyrroles - pharmacology</subject><subject>Rats</subject><subject>Sarcolemma - metabolism</subject><subject>Vertebrates: cardiovascular system</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE2LFDEQhoMo67j6DxRyENFDr1Xp7vTkIujgx8LAgqwgiIR81DiR7mQ26Vnw35txhvW2pzq8TxVvPYw9R7hAQPkWAGQjFH5_rcQbhXLAZvWALRAUNAKhe8gWd8hj9qSU3wCInVRn7AwlQtv3C3ZzvSW-S7MpJewn7rYmRhp52lGkzD98XfN2KcTAQ9wGG-bCbYg-xF88bfgPjqK__NmMxtI4kucUfZq3NIbYIJ8Tz2bmzmQfjOMTTTabSOUpe7QxY6Fnp3nOvn36eL360qyvPl-u3q8b1y7l3JD3RkCnEG19QhqHHlvrSTrVy_YQLjtwtjOgBArjjeqgakHbDzh46dtz9up4d5fTzZ7KrKdQXC1aS6R90UNb-aEXFeyOoMuplEwbvcthMvmPRtAH0_qgUR80aiX0P9N6VddenO7v7UT-_9JRbc1fnnJTnBk39XkXyh3Wt92w7KFi744YVRe3gbIuLlB05EMmN2ufwv09_gLDaZhv</recordid><startdate>19920615</startdate><enddate>19920615</enddate><creator>Waugh, Christopher J.</creator><creator>Dockrell, Mark E.C.</creator><creator>Haynes, William G.</creator><creator>Olverman, Henry J.</creator><creator>Williams, Brent C.</creator><creator>Webb, David J.</creator><general>Elsevier Inc</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>7X8</scope></search><sort><creationdate>19920615</creationdate><title>The potassium channel opener BRL 38227 inhibits binding of [ 125I]-labelled endothelin-1 to rat cardiac membranes</title><author>Waugh, Christopher J. ; Dockrell, Mark E.C. ; Haynes, William G. ; Olverman, Henry J. ; Williams, Brent C. ; Webb, David J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-edda204911b0066ac1d13bde6c9563dda2840cb4a09212ada9401011b5717d6d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1992</creationdate><topic>Animals</topic><topic>Benzopyrans - metabolism</topic><topic>Benzopyrans - pharmacology</topic><topic>Binding, Competitive</topic><topic>Biological and medical sciences</topic><topic>Blood vessels and receptors</topic><topic>Cromakalim</topic><topic>Endothelins - metabolism</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>In Vitro Techniques</topic><topic>Ion Channel Gating - drug effects</topic><topic>Myocardium - metabolism</topic><topic>Nifedipine - pharmacology</topic><topic>Potassium Channels - drug effects</topic><topic>Pyrroles - metabolism</topic><topic>Pyrroles - pharmacology</topic><topic>Rats</topic><topic>Sarcolemma - metabolism</topic><topic>Vertebrates: cardiovascular system</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Waugh, Christopher J.</creatorcontrib><creatorcontrib>Dockrell, Mark E.C.</creatorcontrib><creatorcontrib>Haynes, William G.</creatorcontrib><creatorcontrib>Olverman, Henry J.</creatorcontrib><creatorcontrib>Williams, Brent C.</creatorcontrib><creatorcontrib>Webb, David 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>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Waugh, Christopher J.</au><au>Dockrell, Mark E.C.</au><au>Haynes, William G.</au><au>Olverman, Henry J.</au><au>Williams, Brent C.</au><au>Webb, David J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The potassium channel opener BRL 38227 inhibits binding of [ 125I]-labelled endothelin-1 to rat cardiac membranes</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>1992-06-15</date><risdate>1992</risdate><volume>185</volume><issue>2</issue><spage>630</spage><epage>635</epage><pages>630-635</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><coden>BBRCA9</coden><abstract>Binding of [
125I]-labelled endothelin-1 (ET-1) to rat cardiac membranes and the effects of endothelin-1 (ET-1), endothelin-3 (ET-3), the calcium channel antagonist nifedipine, and both enantiomers of the potassium channel opener cromakalim (BRL 34915) on binding have been examined. Specific binding of [
125I]-ET-1 was inhibited in a concentration dependent manner by both unlabelled ET-1 (10
−12 – 10
−7 M) and ET-3 (10
−12 – 10
−6 M). Nifedipine (10
−11 – 10
−5 M) did not affect [
125I]-ET-1 binding. However, BRL 38227 (10
−11 – 10
−5 M), the biologically active isomer of cromakalim, significantly inhibited [
125I]-ET-1 binding. The inactive isomer, BRL 38226 (10
−11 – 10
−5 M) had no effect. These findings provide the first evidence for a stereospecific interaction between BRL 38227 and an ET-1 binding site in rat cardiac membranes.</abstract><cop>San Diego, CA</cop><pub>Elsevier Inc</pub><pmid>1610355</pmid><doi>10.1016/0006-291X(92)91671-C</doi><tpages>6</tpages></addata></record> |
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| ispartof | Biochemical and biophysical research communications, 1992-06, Vol.185 (2), p.630-635 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Animals Benzopyrans - metabolism Benzopyrans - pharmacology Binding, Competitive Biological and medical sciences Blood vessels and receptors Cromakalim Endothelins - metabolism Fundamental and applied biological sciences. Psychology In Vitro Techniques Ion Channel Gating - drug effects Myocardium - metabolism Nifedipine - pharmacology Potassium Channels - drug effects Pyrroles - metabolism Pyrroles - pharmacology Rats Sarcolemma - metabolism Vertebrates: cardiovascular system |
| title | The potassium channel opener BRL 38227 inhibits binding of [ 125I]-labelled endothelin-1 to rat cardiac membranes |
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