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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
1997-6-17
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pubmed:abstractText |
Progesterone and its A-ring reduced metabolites are allosteric activators of GABA(A) receptors. The studies reported here examined the effects of these steroids on brain nicotinic receptors using an 86Rb+ efflux assay that likely measures the function of alpha4beta2-type nicotinic receptors and [3H]dopamine release, which may be modulated by an alpha3-containing nicotinic receptor. Both of the A-ring reduced metabolites of progesterone were noncompetitive inhibitors of both assays, whereas progesterone inhibited only the 86Rb+ efflux assay. The 86Rb+ efflux assay was slightly more sensitive than was the dopamine release assay to steroid inhibition. Inhibition developed slowly for both assays (t1/2 = 0.4 min) and was reversed even more slowly (t1/2 = 10-15 min). Steroid addition did not alter either the rate of association of [3H]nicotine binding to brain membranes, nor was equilibrium binding changed. These findings argue that neurosteroids are allosteric inhibitors of brain nicotinic receptors.
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pubmed:grant |
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/5-alpha-Dihydroprogesterone,
http://linkedlifedata.com/resource/pubmed/chemical/Anticonvulsants,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotine,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotinic Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Pregnanediones,
http://linkedlifedata.com/resource/pubmed/chemical/Pregnanolone,
http://linkedlifedata.com/resource/pubmed/chemical/Progesterone,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Nicotinic,
http://linkedlifedata.com/resource/pubmed/chemical/Rubidium Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0022-3042
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
68
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2412-23
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:9166735-5-alpha-Dihydroprogesterone,
pubmed-meshheading:9166735-Allosteric Regulation,
pubmed-meshheading:9166735-Animals,
pubmed-meshheading:9166735-Anticonvulsants,
pubmed-meshheading:9166735-Dopamine,
pubmed-meshheading:9166735-Dose-Response Relationship, Drug,
pubmed-meshheading:9166735-Female,
pubmed-meshheading:9166735-Mice,
pubmed-meshheading:9166735-Mice, Inbred C3H,
pubmed-meshheading:9166735-Neostriatum,
pubmed-meshheading:9166735-Nicotine,
pubmed-meshheading:9166735-Nicotinic Agonists,
pubmed-meshheading:9166735-Pregnanediones,
pubmed-meshheading:9166735-Pregnanolone,
pubmed-meshheading:9166735-Progesterone,
pubmed-meshheading:9166735-Receptors, Nicotinic,
pubmed-meshheading:9166735-Rubidium Radioisotopes,
pubmed-meshheading:9166735-Synaptosomes,
pubmed-meshheading:9166735-Thalamus,
pubmed-meshheading:9166735-Tritium
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pubmed:year |
1997
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pubmed:articleTitle |
Neurosteroids modulate nicotinic receptor function in mouse striatal and thalamic synaptosomes.
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pubmed:affiliation |
Institute for Behavioral Genetics, University of Colorado, Boulder 80309-0447, U.S.A.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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