Inhibitory Effects of Corymine-Related Compounds on Glycine Receptors Expressed in Xenopus Oocytes
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We examined the effects of 4 corymine-related compounds on glycine-induced chloride current in <I>Xenopus</I> oocytes. Dihydrocorymine, <I>N</I>-demethyl-3-epi-dihydrocorymine and deformylcorymine dose-dependently decreased the glycine current with IC<SUB>50</SUB> values of 34, 37 and 55 μM, respectively. The effect of these compounds on the glycine current was more potent than that of pleiocarpamine (IC<SUB>50</SUB> > 1 mM). <I>N</I>-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.
- The Japanese Journal of Pharmacology
The Japanese Journal of Pharmacology 77(2), 169-172, 1998-06-01
The Japanese Pharmacological Society