Selective potentiation of alpha 1 glycine receptors by ginkgolic acid
作者： Galyna Maleeva , Svetlana Buldakova , Piotr Bregestovski
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摘要: Glycine receptors (GlyRs) belong to the superfamily of pentameric cys-loop receptor-operated channels and are involved in numerous physiological functions, including movement, vision pain. In search for compounds performing subunit-specific modulation GlyRs we studied action ginkgolic acid, an abundant Ginkgo biloba product. Using patch-clamp recordings, analysed effects acid concentrations from 30nM 25µM on α1- α3 α1/β configurations GlyR GABAARs expressed cultured CHO-K1 cells mouse neuroblastoma (N2a) cells. Ginkgolic caused increase amplitude currents mediated by homomeric α1 heteromeric provoked a left-shift concentration-dependent curves glycine. Even at high (10-25 µM) was not able augment ionic α2 GlyRs, or GABAAR consisting α1/β2/γ2 subunits. Mutation three residues (T59A/A261G/A303S) subunit corresponding ones converted potentiation with distinct decrease EC50 glycine, suggesting important role these acid. Our results suggest that is novel selective enhancer
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