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XB-ART-3385
Eur J Pharmacol 2004 Jun 28;4942-3:131-8. doi: 10.1016/j.ejphar.2004.04.051.
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Ginkgolides, diterpene trilactones of Ginkgo biloba, as antagonists at recombinant alpha1beta2gamma2L GABAA receptors.

Huang SH , Duke RK , Chebib M , Sasaki K , Wada K , Johnston GA .


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Ginkgolides A, B, and C are diterpene trilactones and active constituents of the 50:1 Ginkgo biloba leaf extract widely used in the symptomatic treatment of mild to moderate dementia. Using the two-electrode voltage clamp methodology, these ginkgolides were found to be moderately potent antagonists at recombinant human alpha(1)beta(2)gamma(2L) GABA(A) receptors expressed in Xenopus oocytes. Ginkgolides A, B, and C inhibited the direct action of gamma-aminobutyric acid (GABA) with K(i) values of 14.5+/-1.0, 12.7+/-1.7, and 16.3+/-2.4 microM respectively. Antagonism by these ginkgolides at alpha(1)beta(2)gamma(2L) GABA(A) receptors appears to be noncompetitive as indicated by the nonparallel right shift and reduced maximal GABA response in their GABA concentration-effect curves.

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Species referenced: Xenopus laevis
Genes referenced: gabarap