Inhibition of Na+‐dependent Ca2+ efflux from heart mitochondria by amiloride analogues
The Na+‐induced release of accumulated Ca2+ from heart mitochondria is inhibited by amiloride, benzamil and several other amiloride analogues. These drugs do not affect uptake or release of Ca2+ mediated by the ruthenium red‐sensitive uniporter and their effects, like those of diltiazem and other Ca...
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| Veröffentlicht in: | FEBS letters 1983-10, Vol.162 (2), p.262-265 |
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| container_title | FEBS letters |
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| creator | Jurkowitz, Marianne S. Altschuld, Ruth A. Brierley, Gerald P. Cragoe, Edward J. |
| description | The Na+‐induced release of accumulated Ca2+ from heart mitochondria is inhibited by amiloride, benzamil and several other amiloride analogues. These drugs do not affect uptake or release of Ca2+ mediated by the ruthenium red‐sensitive uniporter and their effects, like those of diltiazem and other Ca2+‐antagonists, appear to be localized principally at the Na+/Ca2+ antiporter of the mitochondrion. Benzamil inhibits Na+/Ca2+ antiport non‐competitively with respect to [Na+] with a K
i of 167 μM. In the presence of 1.5 mM Pi the K
i for benzamil inhibition of this reaction is decreased to 87 μM. |
| doi_str_mv | 10.1016/0014-5793(83)80768-6 |
| format | Article |
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i of 167 μM. In the presence of 1.5 mM Pi the K
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i of 167 μM. In the presence of 1.5 mM Pi the K
i for benzamil inhibition of this reaction is decreased to 87 μM.</description><subject>Amiloride</subject><subject>Amiloride - analogs & derivatives</subject><subject>Amiloride - pharmacology</subject><subject>Animals</subject><subject>Benzamil</subject><subject>Biological and medical sciences</subject><subject>Biological Transport, Active - drug effects</subject><subject>Ca2+ antagonist</subject><subject>Calcium - metabolism</subject><subject>Cattle</subject><subject>Cell physiology</subject><subject>Diltiazem</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>In Vitro Techniques</subject><subject>Membrane and intracellular transports</subject><subject>Mitochondria, Heart - metabolism</subject><subject>Mitochondrial Na+/Ca2+ antiporter</subject><subject>Molecular and cellular biology</subject><subject>Pyrazines - pharmacology</subject><subject>Sodium - physiology</subject><issn>0014-5793</issn><issn>1873-3468</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1983</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kcFKxDAQhoMouq6-gUIOIopUk6aZpkddXBVELwreQpJO3UjbrG0X3ZuP4DP6JLa67GmY__-Ygf8n5ICzc844XDDGk0immThR4lSxFFQEG2TEVSoikYDaJKM1skN22_aN9bvi2TbZBogVpGxEXu7qmbe-86GmoaAP5uzn6zvHOdY51h2dmPiMYlGUi09aNKGiMzRNRyvfBTcLdd54Q-2SmsqXofE5UlObMrwusN0jW4UpW9xfzTF5nl4_TW6j-8ebu8nlfTTniYRIKgDMwaIDG3NpLIATqEwaJ8AsFg4Y5hItxtaBERAnhZU2V0oCOkylGJPj_7vzJrz3fztd-dZhWZoaw6LVfTAM0izrwcMVuLAV5nre-Mo0S72KovePVr5pnSmLxtTOt2ssS5Ikk7zHpv_Yhy9xubY500MpekhcD4lrJfRfKRr09PoqHoxBV-JPBfELdt-CzQ</recordid><startdate>19831017</startdate><enddate>19831017</enddate><creator>Jurkowitz, Marianne S.</creator><creator>Altschuld, Ruth A.</creator><creator>Brierley, Gerald P.</creator><creator>Cragoe, Edward J.</creator><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>7X8</scope></search><sort><creationdate>19831017</creationdate><title>Inhibition of Na+‐dependent Ca2+ efflux from heart mitochondria by amiloride analogues</title><author>Jurkowitz, Marianne S. ; Altschuld, Ruth A. ; Brierley, Gerald P. ; Cragoe, Edward J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p1456-5866ed6bec6b215ab66c3e8a72460befc60ed5ebe2bc6a3624fb5bd8856ece753</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1983</creationdate><topic>Amiloride</topic><topic>Amiloride - analogs & derivatives</topic><topic>Amiloride - pharmacology</topic><topic>Animals</topic><topic>Benzamil</topic><topic>Biological and medical sciences</topic><topic>Biological Transport, Active - drug effects</topic><topic>Ca2+ antagonist</topic><topic>Calcium - metabolism</topic><topic>Cattle</topic><topic>Cell physiology</topic><topic>Diltiazem</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>In Vitro Techniques</topic><topic>Membrane and intracellular transports</topic><topic>Mitochondria, Heart - metabolism</topic><topic>Mitochondrial Na+/Ca2+ antiporter</topic><topic>Molecular and cellular biology</topic><topic>Pyrazines - pharmacology</topic><topic>Sodium - physiology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jurkowitz, Marianne S.</creatorcontrib><creatorcontrib>Altschuld, Ruth A.</creatorcontrib><creatorcontrib>Brierley, Gerald P.</creatorcontrib><creatorcontrib>Cragoe, Edward 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>MEDLINE - Academic</collection><jtitle>FEBS letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Jurkowitz, Marianne S.</au><au>Altschuld, Ruth A.</au><au>Brierley, Gerald P.</au><au>Cragoe, Edward J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibition of Na+‐dependent Ca2+ efflux from heart mitochondria by amiloride analogues</atitle><jtitle>FEBS letters</jtitle><addtitle>FEBS Lett</addtitle><date>1983-10-17</date><risdate>1983</risdate><volume>162</volume><issue>2</issue><spage>262</spage><epage>265</epage><pages>262-265</pages><issn>0014-5793</issn><eissn>1873-3468</eissn><coden>FEBLAL</coden><abstract>The Na+‐induced release of accumulated Ca2+ from heart mitochondria is inhibited by amiloride, benzamil and several other amiloride analogues. These drugs do not affect uptake or release of Ca2+ mediated by the ruthenium red‐sensitive uniporter and their effects, like those of diltiazem and other Ca2+‐antagonists, appear to be localized principally at the Na+/Ca2+ antiporter of the mitochondrion. Benzamil inhibits Na+/Ca2+ antiport non‐competitively with respect to [Na+] with a K
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i for benzamil inhibition of this reaction is decreased to 87 μM.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>6628670</pmid><doi>10.1016/0014-5793(83)80768-6</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-5793 |
| ispartof | FEBS letters, 1983-10, Vol.162 (2), p.262-265 |
| issn | 0014-5793 1873-3468 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_80706799 |
| source | MEDLINE; Access via ScienceDirect (Elsevier); EZB-FREE-00999 freely available EZB journals; Alma/SFX Local Collection |
| subjects | Amiloride Amiloride - analogs & derivatives Amiloride - pharmacology Animals Benzamil Biological and medical sciences Biological Transport, Active - drug effects Ca2+ antagonist Calcium - metabolism Cattle Cell physiology Diltiazem Fundamental and applied biological sciences. Psychology In Vitro Techniques Membrane and intracellular transports Mitochondria, Heart - metabolism Mitochondrial Na+/Ca2+ antiporter Molecular and cellular biology Pyrazines - pharmacology Sodium - physiology |
| title | Inhibition of Na+‐dependent Ca2+ efflux from heart mitochondria by amiloride analogues |
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