Picrodendrins, a New Group of Picrotoxane Terpenoids: Structure-Activity Profile of Action at the GABAA Receptor-coupled Picrotoxinin Binding Site in Rat Brain.

Ozoe Yoshihisa, Hasegawa Hiroko, Mochida Kazuo, Koike Kazuo, Suzuki Yumiko, Nagahisa Masako, Ohmoto Taichi

doi:10.1271/bbb.58.1506

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Picrodendrins, a New Group of Picrotoxane Terpenoids: Structure-Activity Profile of Action at the GABA<sub>A</sub>Receptor-coupled Picrotoxinin Binding Site in Rat Brain

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Description

Seven out of 20 assayed picrotoxane terpenoids inhibited specific binding of [³⁵S] t-butylbicyclophosphorothionate to rat brain membranes, with IC₅₀ values of 0. 0075-6. 0μM. Picrodendrin Q was identified as the most potent compound, being about 27-fold more potent than picrotoxinin. The high activity of picrodendrins A, M, and Q suggests the significance of the spiro α-ethylidene γ-lactone moiety for the interaction of picrodendrins with the GABAA receptor-coupled picrotoxinin binding site.

Journal

Bioscience, Biotechnology, and Biochemistry

Bioscience, Biotechnology, and Biochemistry 58 (8), 1506-1507, 1994

Japan Society for Bioscience, Biotechnology, and Agrochemistry

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Details 詳細情報について

CRID: 1390282681452620160

NII Article ID: 110002677129

NII Book ID: AA10824164

DOI: 10.1271/bbb.58.1506

ISSN: 13476947; 09168451

Web Site: http://www.tandfonline.com/doi/pdf/10.1271/bbb.58.1506; https://search.jamas.or.jp/link/ui/1995075710

Text Lang: en

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