Effects of a new centrally acting muscle relaxant, NK433 (lanperisone hydrochloride) on spinal reflexes

European Journal of Pharmacology
K SakitamaM Ishikawa

Abstract

(-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'-trifluoromethylpropiophenone++ + monohydrochloride, lanperisone hydrochloride (NK433) administered intravenously or orally depressed the mono- and polysynaptic reflex potential, dorsal root reflex potential, flexor reflex mediated by group II afferent fibers, patellar and flexor reflexes. These effects were reduced by spinal transection. NK433 inhibited the facilitation of the flexor reflex mediated by group II afferent fibers that was induced by intrathecal administration of noradrenaline-HCl. (+)-(1R,2R)-2-methyl-3-(1-pyrrolidinyl)-1-(4-trifluoromethylphenyl)-1-pr opanol (LPS-9)-HCl, a metabolite of NK433, also inhibited the spinal reflexes. Given orally, NK433 had effects more than three times stronger and tending to be longer-lasting than those of eperisone-HCl. These results suggest that NK433 exerts a non-selective inhibition on spinal reflexes and that inhibition of the descending noradrenergic tonic facilitation within the spinal cord is involved in the mechanism of spinal reflex depression by NK433. LPS-9 could contribute to the potent activity of NK433 after oral administration.

References

Oct 1, 1992·Japanese Journal of Pharmacology·K Sakitama, M Ishikawa
Jul 1, 1990·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·H Fukuda, H Ono
Jan 1, 1974·Naunyn-Schmiedeberg's Archives of Pharmacology·P PolcW Haefely
Jan 1, 1972·Brain : a Journal of Neurology·R Garcia-Mullin, R F Mayer
Jan 24, 1995·European Journal of Pharmacology·K SakitamaM Ishikawa

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Citations

May 11, 2011·Proceedings of the National Academy of Sciences of the United States of America·Alice T ShawTyler Jacks
Jan 23, 2016·Cell Death and Differentiation·Y XieD Tang
May 17, 2008·CNS Neuroscience & Therapeutics·Stefan QuasthoffWolfgang Schreibmayer
Sep 27, 2012·Expert Opinion on Therapeutic Patents·Elena SaccoMarco Vanoni
Aug 30, 2005·The Journal of Pharmacology and Experimental Therapeutics·Pál KocsisIstván Tarnawa
Jun 1, 2011·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Hye Hyun YooDong-Hyun Kim

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