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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 |
2005-6-6
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pubmed:abstractText |
The ionophore function of gamma-aminobutyric acid A (GABA(A)) receptors was studied by whole-cell patch clamp electrophysiology in primary cultures of rat cerebellar cortex. Chloride currents elicited by 1 microM GABA were potentiated by allopregnanolone with a plateau of high affinity (EC(50) = 14 nM) and a peak of potentiation around 1 microM allopregnanolone. Furosemide (0.1 mM) eliminated the high affinity phase and increased the EC(50) to 685 nM. GABA(A) receptors of rat cerebellar synaptosomal membranes were labelled with [(3)H]ethynylbicycloorthobenzoate (EBOB). Allopregnanolone displaced [(3)H]EBOB binding with IC(50) = 320 nM. The displacing potency of allopregnanolone was strongly enhanced (IC(50) = 39 nM) in the presence of 400 nM GABA and 60 nM SR 95531. Nanomolar potentiation by allopregnanolone can be associated with cerebellar GABA(A) receptors containing alpha(6), beta(2-3) and delta subunits. This might be suitable for physiological modulation of tonic inhibitory neurotransmission via extrasynaptic GABA(A) receptors in cerebellar granule cells by neurosteroids.
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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/1-(4-ethynylphenyl)-4-propyl-2,6,7-t...,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds, Heterocyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Chlorides,
http://linkedlifedata.com/resource/pubmed/chemical/Furosemide,
http://linkedlifedata.com/resource/pubmed/chemical/GABA Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Pregnanolone,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A,
http://linkedlifedata.com/resource/pubmed/chemical/gabazine,
http://linkedlifedata.com/resource/pubmed/chemical/gamma-Aminobutyric Acid
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pubmed:status |
MEDLINE
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pubmed:issn |
0304-3940
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
383
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
127-30
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15936524-Analysis of Variance,
pubmed-meshheading:15936524-Animals,
pubmed-meshheading:15936524-Animals, Newborn,
pubmed-meshheading:15936524-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:15936524-Binding, Competitive,
pubmed-meshheading:15936524-Cells, Cultured,
pubmed-meshheading:15936524-Cerebellar Cortex,
pubmed-meshheading:15936524-Chlorides,
pubmed-meshheading:15936524-Dose-Response Relationship, Drug,
pubmed-meshheading:15936524-Drug Interactions,
pubmed-meshheading:15936524-Furosemide,
pubmed-meshheading:15936524-GABA Antagonists,
pubmed-meshheading:15936524-Membrane Potentials,
pubmed-meshheading:15936524-Neurons,
pubmed-meshheading:15936524-Patch-Clamp Techniques,
pubmed-meshheading:15936524-Pregnanolone,
pubmed-meshheading:15936524-Pyridazines,
pubmed-meshheading:15936524-Rats,
pubmed-meshheading:15936524-Rats, Wistar,
pubmed-meshheading:15936524-Receptors, GABA-A,
pubmed-meshheading:15936524-gamma-Aminobutyric Acid
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pubmed:articleTitle |
Nanomolar allopregnanolone potentiates rat cerebellar GABAA receptors.
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pubmed:affiliation |
Pharmacological Research, Gedeon Richter Ltd., Budapest, Hungary.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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