Detail of "15291-78-8"

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Terpene Trilactones from Ginkgo biloba Are Antagonists of Cortical Glycine and GABAA Receptors

Terpene Trilactones from Ginkgo biloba Are Antagonists of Cortical Glycine and GABAA Receptors. Ivic, Lidija; Sands, Tristan T. J.; Fishkin, Nathan; Nakanishi, Koji; Kriegstein, Arnold R.; Stromgaard, Kristian (College of Physicians & Surgeons and the Integrated Program in Cellular, Department of Neurology, Columbia University, new york, NY 10032, USA). Journal of Biological Chemistry, 278(49), 49279-49285 (English) 2003 American Society for Biochemistry and Molecular Biology. CODEN: JBCHA3. ISSN: 0021-9258. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Glycine and g-aminobutyric acid, type A (GABAA) receptors are members of the ligand-gated ion channel superfamily that mediate inhibitory synaptic transmission in the adult central nervous system. During development, the activation of these receptors leads to membrane depolarization. Ligands for the two receptors have important implications both in disease therapy and as pharmacol. tools. Terpene trilactones (ginkgolides and bilobalide) are unique constituents of Ginkgo biloba exts. that have various effects on the central nervous system. We have investigated the relative potency of these compds. on glycine and GABAA receptors.Several substances with their cas registry numbers 15291-78-8 and 15291-77-7 may be metioned in this study. We find that most of the ginkgolides are selective and potent antagonists of the glycine receptor. Bilobalide, the single major component in G. biloba exts., also reduces glycine-induced currents, although to a lesser extent. Both ginkgolides and bilobalide inhibit GABAA receptors, with bilobalide demonstrating a more potent effect. Addnl., we provide evidence that open channels are required for glycine receptor inhibition by ginkgolides. Finally, we employ mol. modeling to elucidate the similarities and differences in the structure of the terpene trilactones to account for the pharmacol. properties of these compds. and demonstrate a striking similarity between ginkgolides and picrotoxinin, a GABAA and recombinant glycine a-homomeric receptor antagonist. .