The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Short Communications
Inhibitory Effects of Corymine-Related Compounds on Glycine Receptors Expressed in Xenopus Oocytes
Pathama LeewanichMichihisa TohdaKinzo MatsumotoSanan SubhadhirasakulHiromitsu TakayamaNorio AimiHiroshi Watanabe
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1998 Volume 77 Issue 2 Pages 169-172

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Abstract

We examined the effects of 4 corymine-related compounds on glycine-induced chloride current in Xenopus oocytes. Dihydrocorymine, N-demethyl-3-epi-dihydrocorymine and deformylcorymine dose-dependently decreased the glycine current with IC50 values of 34, 37 and 55 μM, respectively. The effect of these compounds on the glycine current was more potent than that of pleiocarpamine (IC50 > 1 mM). N-Demethyl-3-epi-dihydrocorymine and dihydrocorymine, at 100 μM, also decreased the γ-aminobutyric acid-induced current by 65% and 22%, respectively, whereas deformylcorymine and pleiocarpamine failed. The inhibitory action of deformylcorymine on the glycine current was noncompetitive. These results suggest that deformylcorymine is a novel specific noncompetitive glycine receptor antagonist. The structure-activity relationship of these compounds was discussed.

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© The Japanese Pharmacological Society 1998
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