Specific inhibition of Ca‐activated K channels in red cells by selected dihydropyridine derivatives
1 Thirty two dihydropyridine derivatives were screened as potential inhibitors of the Ca‐activated K‐channel in human red cells. 2 Three derivatives (26, 29, 32 see Tables 1 and 2) with high activity were then characterized in detail, and also tested against the smooth muscle Ca‐channel and shown to...
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| Veröffentlicht in: | British journal of pharmacology 1994-03, Vol.111 (3), p.903-905 |
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| container_title | British journal of pharmacology |
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| creator | Ellory, J.C. Culliford, S.J. Smith, P.A. Wolowyk, M.W. Knaus, E.E. |
| description | 1
Thirty two dihydropyridine derivatives were screened as potential inhibitors of the Ca‐activated K‐channel in human red cells.
2
Three derivatives (26, 29, 32 see Tables 1 and 2) with high activity were then characterized in detail, and also tested against the smooth muscle Ca‐channel and shown to have varying potencies.
3
One of the more potent derivatives (32) and nitrendipine were also tested on the Ca‐activated K‐channel, Maxi‐K channel, from mouse pancreatic beta‐cells.
4
We conclude from our results that it may be possible to develop selective Gardos‐channel inhibitors based on these molecules, which may be of benefit in the treatment of sickle cell disease. |
| doi_str_mv | 10.1111/j.1476-5381.1994.tb14823.x |
| format | Article |
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Thirty two dihydropyridine derivatives were screened as potential inhibitors of the Ca‐activated K‐channel in human red cells.
2
Three derivatives (26, 29, 32 see Tables 1 and 2) with high activity were then characterized in detail, and also tested against the smooth muscle Ca‐channel and shown to have varying potencies.
3
One of the more potent derivatives (32) and nitrendipine were also tested on the Ca‐activated K‐channel, Maxi‐K channel, from mouse pancreatic beta‐cells.
4
We conclude from our results that it may be possible to develop selective Gardos‐channel inhibitors based on these molecules, which may be of benefit in the treatment of sickle cell disease.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1994.tb14823.x</identifier><identifier>PMID: 8019767</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Biological and medical sciences ; Blood. Blood coagulation. Reticuloendothelial system ; Calcium - physiology ; Dihydropyridine ; Dihydropyridines - pharmacology ; erythrocyte ; Erythrocytes - chemistry ; gardos channel ; Humans ; ileal smooth muscle ; L‐type Ca‐channel ; maxi‐K channel ; Medical sciences ; Nitrendipine - pharmacology ; Pharmacology. Drug treatments ; Potassium Channel Blockers ; Potassium Channels - blood ; Potassium Channels - drug effects ; β‐cell</subject><ispartof>British journal of pharmacology, 1994-03, Vol.111 (3), p.903-905</ispartof><rights>1994 British Pharmacological Society</rights><rights>1994 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5073-f53fcc35cf9dca920f0b599ec62e5e4dd1639bbfd626fbb0dbe05cc91a0626583</citedby><cites>FETCH-LOGICAL-c5073-f53fcc35cf9dca920f0b599ec62e5e4dd1639bbfd626fbb0dbe05cc91a0626583</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/PMC1910101/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1910101/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3963567$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8019767$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ellory, J.C.</creatorcontrib><creatorcontrib>Culliford, S.J.</creatorcontrib><creatorcontrib>Smith, P.A.</creatorcontrib><creatorcontrib>Wolowyk, M.W.</creatorcontrib><creatorcontrib>Knaus, E.E.</creatorcontrib><title>Specific inhibition of Ca‐activated K channels in red cells by selected dihydropyridine derivatives</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
Thirty two dihydropyridine derivatives were screened as potential inhibitors of the Ca‐activated K‐channel in human red cells.
2
Three derivatives (26, 29, 32 see Tables 1 and 2) with high activity were then characterized in detail, and also tested against the smooth muscle Ca‐channel and shown to have varying potencies.
3
One of the more potent derivatives (32) and nitrendipine were also tested on the Ca‐activated K‐channel, Maxi‐K channel, from mouse pancreatic beta‐cells.
4
We conclude from our results that it may be possible to develop selective Gardos‐channel inhibitors based on these molecules, which may be of benefit in the treatment of sickle cell disease.</description><subject>Biological and medical sciences</subject><subject>Blood. Blood coagulation. Reticuloendothelial system</subject><subject>Calcium - physiology</subject><subject>Dihydropyridine</subject><subject>Dihydropyridines - pharmacology</subject><subject>erythrocyte</subject><subject>Erythrocytes - chemistry</subject><subject>gardos channel</subject><subject>Humans</subject><subject>ileal smooth muscle</subject><subject>L‐type Ca‐channel</subject><subject>maxi‐K channel</subject><subject>Medical sciences</subject><subject>Nitrendipine - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Potassium Channel Blockers</subject><subject>Potassium Channels - blood</subject><subject>Potassium Channels - drug effects</subject><subject>β‐cell</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkc9u1DAQxi1EVbaFR0CKEOKWYMdxEnNAwIrSikogAWfLf8asV1lna2e3zY1H4Bl5kjrdaAVH7IPH8_1mPNaH0AuCC5LW63VBqqbOGW1JQTivikGRqi1pcfcILY7SY7TAGDc5IW37BJ3FuMY4iQ07RactJrypmwWCb1vQzjqdOb9yyg2u91lvs6X88-u31IPbywFM9jnTK-k9dDFxWUgZDV26qDGL0IGeGONWown9dgzOOA-ZgTBVuz3Ep-jEyi7Cs_k8Rz8uPn5fXubXXz5dLd9f55rhhuaWUas1ZdpyoyUvscWKcQ66LoFBZQypKVfKmrqsrVLYKMBMa04kThnW0nP09tB3u1MbMBr8EGQntsFtZBhFL534V_FuJX72e0E4wWmnBq_mBqG_2UEcxMbF6avSQ7-LoqkZa8q2SuCbA6hDH2MAe3yEYDGZJNZickJMTojJJDGbJO5S8fO_xzyWzq4k_eWsy6hlZ4P02sUjRnlN2QP27oDdug7G_xhAfPh6-RDSe0UIs60</recordid><startdate>199403</startdate><enddate>199403</enddate><creator>Ellory, J.C.</creator><creator>Culliford, S.J.</creator><creator>Smith, P.A.</creator><creator>Wolowyk, M.W.</creator><creator>Knaus, E.E.</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>199403</creationdate><title>Specific inhibition of Ca‐activated K channels in red cells by selected dihydropyridine derivatives</title><author>Ellory, J.C. ; Culliford, S.J. ; Smith, P.A. ; Wolowyk, M.W. ; Knaus, E.E.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5073-f53fcc35cf9dca920f0b599ec62e5e4dd1639bbfd626fbb0dbe05cc91a0626583</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>Biological and medical sciences</topic><topic>Blood. Blood coagulation. Reticuloendothelial system</topic><topic>Calcium - physiology</topic><topic>Dihydropyridine</topic><topic>Dihydropyridines - pharmacology</topic><topic>erythrocyte</topic><topic>Erythrocytes - chemistry</topic><topic>gardos channel</topic><topic>Humans</topic><topic>ileal smooth muscle</topic><topic>L‐type Ca‐channel</topic><topic>maxi‐K channel</topic><topic>Medical sciences</topic><topic>Nitrendipine - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Potassium Channel Blockers</topic><topic>Potassium Channels - blood</topic><topic>Potassium Channels - drug effects</topic><topic>β‐cell</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ellory, J.C.</creatorcontrib><creatorcontrib>Culliford, S.J.</creatorcontrib><creatorcontrib>Smith, P.A.</creatorcontrib><creatorcontrib>Wolowyk, M.W.</creatorcontrib><creatorcontrib>Knaus, E.E.</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>Ellory, J.C.</au><au>Culliford, S.J.</au><au>Smith, P.A.</au><au>Wolowyk, M.W.</au><au>Knaus, E.E.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Specific inhibition of Ca‐activated K channels in red cells by selected dihydropyridine derivatives</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1994-03</date><risdate>1994</risdate><volume>111</volume><issue>3</issue><spage>903</spage><epage>905</epage><pages>903-905</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>1
Thirty two dihydropyridine derivatives were screened as potential inhibitors of the Ca‐activated K‐channel in human red cells.
2
Three derivatives (26, 29, 32 see Tables 1 and 2) with high activity were then characterized in detail, and also tested against the smooth muscle Ca‐channel and shown to have varying potencies.
3
One of the more potent derivatives (32) and nitrendipine were also tested on the Ca‐activated K‐channel, Maxi‐K channel, from mouse pancreatic beta‐cells.
4
We conclude from our results that it may be possible to develop selective Gardos‐channel inhibitors based on these molecules, which may be of benefit in the treatment of sickle cell disease.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>8019767</pmid><doi>10.1111/j.1476-5381.1994.tb14823.x</doi><tpages>3</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central; Alma/SFX Local Collection |
| subjects | Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Calcium - physiology Dihydropyridine Dihydropyridines - pharmacology erythrocyte Erythrocytes - chemistry gardos channel Humans ileal smooth muscle L‐type Ca‐channel maxi‐K channel Medical sciences Nitrendipine - pharmacology Pharmacology. Drug treatments Potassium Channel Blockers Potassium Channels - blood Potassium Channels - drug effects β‐cell |
| title | Specific inhibition of Ca‐activated K channels in red cells by selected dihydropyridine derivatives |
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