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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
18
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pubmed:dateCreated |
1996-10-17
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pubmed:abstractText |
Dequalinium is a potent and selective blocker of the small conductance Ca(2+)-activated K+ (SKCa) channel in rat sympathetic neurones. Analogues of dequalinium possessing 3-6, 8, 10, and 12 methylene groups in the linking chain have been synthesized and tested for inhibition of the afterhyperpolarization in rat sympathetic neurones. The compounds having a 5-12-carbon chain showed very little variation in their activity as SKCa channel blockers. The analogues possessing four and three methylenes exhibited 3- and 8-fold lower potency, respectively, compared with dequalinium. These results are discussed in the context of possible modes of binding of the compounds to the SKCa channel.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
30
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pubmed:volume |
39
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3592-5
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pubmed:dateRevised |
2009-9-29
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pubmed:meshHeading |
pubmed-meshheading:8784458-Action Potentials,
pubmed-meshheading:8784458-Amino Acid Sequence,
pubmed-meshheading:8784458-Animals,
pubmed-meshheading:8784458-Apamin,
pubmed-meshheading:8784458-Calcium,
pubmed-meshheading:8784458-Dequalinium,
pubmed-meshheading:8784458-Ganglia, Sympathetic,
pubmed-meshheading:8784458-Molecular Sequence Data,
pubmed-meshheading:8784458-Potassium Channel Blockers,
pubmed-meshheading:8784458-Rats,
pubmed-meshheading:8784458-Structure-Activity Relationship
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pubmed:year |
1996
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pubmed:articleTitle |
Synthesis and pharmacological testing of dequalinium analogues as blockers of the apamin-sensitive Ca(2+)-activated K+ channel: variation of the length of the alkylene chain.
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pubmed:affiliation |
Department of Chemistry, University College London, U.K.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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