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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2003-2-25
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pubmed:abstractText |
The sesquiterpene trilactone bilobalide is one of the active constituents of the 50:1 Ginkgo biloba leaf extract widely used to enhance memory and learning. Bilobalide was found to antagonise the direct action of gamma-aminobutyric acid (GABA) on recombinant alpha(1)beta(2)gamma(2L) GABA(A) receptors. The effect of bilobalide on the direct action of GABA at alpha(1)beta(2)gamma(2L) GABA(A) receptors expressed in Xenopus laevis oocytes using two-electrode voltage-clamp method was evaluated and compared with the effects of the classical GABA(A) receptor competitive antagonist bicuculline and noncompetitive antagonist picrotoxinin. Bilobalide (IC(50)=4.6+/-0.5 microM) was almost as potent as bicuculline and pictrotoxinin (IC(50)=2.0+/-0.1 and 2.4+/-0.5 microM, respectively) at alpha(1)beta(2)gamma(2L) GABA(A) receptors against 40 microM GABA (GABA EC(50)). While bilobalide and picrotoxinin were clearly noncompetitive antagonists, the potency of bilobalide decreased at high GABA concentrations suggesting a component of competitive antagonism.
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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/Bicuculline,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclopentanes,
http://linkedlifedata.com/resource/pubmed/chemical/Diterpenes,
http://linkedlifedata.com/resource/pubmed/chemical/Furans,
http://linkedlifedata.com/resource/pubmed/chemical/GABA Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/GABA-A Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Ginkgolides,
http://linkedlifedata.com/resource/pubmed/chemical/Picrotoxin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/bilobalide,
http://linkedlifedata.com/resource/pubmed/chemical/gamma-Aminobutyric Acid,
http://linkedlifedata.com/resource/pubmed/chemical/picrotoxinin
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0014-2999
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
464
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1-8
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:12600688-Animals,
pubmed-meshheading:12600688-Bicuculline,
pubmed-meshheading:12600688-Cyclopentanes,
pubmed-meshheading:12600688-Diterpenes,
pubmed-meshheading:12600688-Dose-Response Relationship, Drug,
pubmed-meshheading:12600688-Furans,
pubmed-meshheading:12600688-GABA Antagonists,
pubmed-meshheading:12600688-GABA-A Receptor Antagonists,
pubmed-meshheading:12600688-Ginkgo biloba,
pubmed-meshheading:12600688-Ginkgolides,
pubmed-meshheading:12600688-Humans,
pubmed-meshheading:12600688-Membrane Potentials,
pubmed-meshheading:12600688-Oocytes,
pubmed-meshheading:12600688-Picrotoxin,
pubmed-meshheading:12600688-Receptors, GABA-A,
pubmed-meshheading:12600688-Recombinant Proteins,
pubmed-meshheading:12600688-Xenopus laevis,
pubmed-meshheading:12600688-gamma-Aminobutyric Acid
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pubmed:year |
2003
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pubmed:articleTitle |
Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors.
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pubmed:affiliation |
Adrien Albert Laboratory of Medicinal Chemistry, Department of Pharmacology, Faculty of Medicine, University of Sydney, NSW 2006, Sydney, Australia.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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