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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1-2
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pubmed:dateCreated |
1996-7-31
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pubmed:abstractText |
The receptor antagonist actions are described for a novel bicyclic dinitrile compound (BIDN, 3,3-bis-(trifluoromethyl)-bicyclo [2.2.1] heptane-2,2-dicarbonitrile) on a Drosophila melanogaster homo-oligomeric GABA receptor expressed in Xenopus oocytes. BIDN blocked the wild-type form of the receptor in a neither purely competitive, nor purely non-competitive manner, being dependent on the GABA concentration yet insurmountable, and block was independent of the membrane potential. BIDN was found to be less effective against a mutant (A(302) --> S) form of the receptor resistant to dieldrin and picrotoxinin. This cross resistance of dieldrin-resistant receptors to BIDN is of interest in the light of recent findings that BIDN binding to insect membranes is displaced competitively by dieldrin, but not by picrotoxinin.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0006-8993
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
693
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
257-60
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8653417-Animals,
pubmed-meshheading:8653417-Bicyclo Compounds,
pubmed-meshheading:8653417-Chloride Channels,
pubmed-meshheading:8653417-Convulsants,
pubmed-meshheading:8653417-Dieldrin,
pubmed-meshheading:8653417-Drosophila melanogaster,
pubmed-meshheading:8653417-Electrophysiology,
pubmed-meshheading:8653417-GABA Antagonists,
pubmed-meshheading:8653417-Gene Expression,
pubmed-meshheading:8653417-Microinjections,
pubmed-meshheading:8653417-Nitriles,
pubmed-meshheading:8653417-Oligopeptides,
pubmed-meshheading:8653417-Oocytes,
pubmed-meshheading:8653417-Receptors, GABA,
pubmed-meshheading:8653417-Xenopus
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pubmed:year |
1995
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pubmed:articleTitle |
Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes.
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pubmed:affiliation |
Babraham Institute Laboratory of Molecular Signalling, Department of Zoology, University of Cambridge, UK.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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