Source:http://linkedlifedata.com/resource/pubmed/id/17161853
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
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| pubmed:dateCreated |
2007-1-26
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| pubmed:abstractText |
The effects of the antipsychotic clozapine on the function of the cloned alpha(7) subunit of the nicotinic acetylcholine (nACh) receptor expressed in Xenopus oocytes was investigated by using the two-electrode voltage-clamp technique. Clozapine reversibly inhibited nicotine (10 microM)-induced currents in a concentration-dependent manner (300 nM to 90 microM), with an IC(50) value of 3.2+/-0.4 microM. The effect of clozapine was not dependent on the membrane potential. Clozapine did not affect the activity of endogenous Ca(2+)-dependent Cl(-) channels since the inhibition by clozapine was unaltered by the intracellularly injected Ca(2+) chelator BAPTA and perfusion with Ca(2+)-free bathing solution containing 2mM Ba(2+). Clozapine decreased the maximal nicotine-induced responses without significantly affecting its potency, indicating that it acts as a noncompetitive antagonist on alpha(7)-nACh receptors. In hippocampal slices, the whole-cell recordings from CA1 pyramidal neurons indicated that the increases in the frequency and amplitudes of the GABA-mediated spontaneous inhibitory postsynaptic currents induced by bath application of 2 mM choline, a specific agonist for alpha(7)-nACh receptors, were abolished after 10 min application of 5 microM clozapine. In conclusion, these results demonstrate that clozapine inhibits the function of alpha(7)-nACh receptors expressed in Xenopus oocytes and in hippocampal neurons.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antipsychotic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Choline,
http://linkedlifedata.com/resource/pubmed/chemical/Clozapine,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotine,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotinic Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Nootropic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Nicotinic,
http://linkedlifedata.com/resource/pubmed/chemical/alpha7 nicotinic acetylcholine...
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| pubmed:status |
MEDLINE
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| pubmed:month |
Feb
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| pubmed:issn |
0028-3908
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
52
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
387-94
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| pubmed:dateRevised |
2010-6-4
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| pubmed:meshHeading |
pubmed-meshheading:17161853-Animals,
pubmed-meshheading:17161853-Animals, Newborn,
pubmed-meshheading:17161853-Antipsychotic Agents,
pubmed-meshheading:17161853-Choline,
pubmed-meshheading:17161853-Clozapine,
pubmed-meshheading:17161853-Dose-Response Relationship, Drug,
pubmed-meshheading:17161853-Dose-Response Relationship, Radiation,
pubmed-meshheading:17161853-Drug Interactions,
pubmed-meshheading:17161853-Female,
pubmed-meshheading:17161853-Hippocampus,
pubmed-meshheading:17161853-Inhibitory Concentration 50,
pubmed-meshheading:17161853-Male,
pubmed-meshheading:17161853-Membrane Potentials,
pubmed-meshheading:17161853-Microinjections,
pubmed-meshheading:17161853-Nicotine,
pubmed-meshheading:17161853-Nicotinic Agonists,
pubmed-meshheading:17161853-Nootropic Agents,
pubmed-meshheading:17161853-Oocytes,
pubmed-meshheading:17161853-Patch-Clamp Techniques,
pubmed-meshheading:17161853-Pyramidal Cells,
pubmed-meshheading:17161853-Rats,
pubmed-meshheading:17161853-Receptors, Nicotinic,
pubmed-meshheading:17161853-Xenopus laevis
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| pubmed:year |
2007
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| pubmed:articleTitle |
Antipsychotic clozapine inhibits the function of alpha7-nicotinic acetylcholine receptors.
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| pubmed:affiliation |
Laboratory of Molecular & Cellular Neurobiology, National Institute on Alcohol Abuse & Alcoholism, NIH/DHHS, 12501 Washington Avenue, Bethesda, MD 20892-8205, USA.
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| pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, N.I.H., Extramural
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