K. Sakitama et al., EFFECTS OF A NEW CENTRALLY ACTING MUSCLE-RELAXANT, NK433 (LANPERISONEHYDROCHLORIDE) ON SPINAL REFLEXES, European journal of pharmacology, 337(2-3), 1997, pp. 175-187
3-(1-pyrrolidinyl)-4'-trifluoromethylpropiophenone monohydrochloride,
lanperisone hydrochloride (NK433) administered intravenously or orally
depressed the mono-and polysynaptic reflex potential, dorsal root ref
lex potential, flexor reflex mediated by group II afferent fibers, pat
ellar and flexor reflexes. These effects were reduced by spinal transe
ction. NK433 inhibited the facilitation of the flexor reflex mediated
by group II afferent fibers that was induced by intrathecal administra
tion of noradrenaline-HCl. rrolidinyl)-1-(4-trifluoromethylphenyl)-1-p
ropano: (LPS-9)-HCl, a metabolite of NK433, also inhibited the spinal
reflexes. Given orally, NK433 had effects more than three times strong
er and tending to be longer-lasting than those of eperisone-HCl. These
results suggest that NK433 exerts a non-selective inhibition on spina
l reflexes and that inhibition of the descending noradrenergic tonic f
acilitation within the spinal cord is involved in the mechanism of spi
nal reflex depression by NK433. LPS-9 could contribute to the potent a
ctivity of NK433 after oral administration. (C) 1997 Elsevier Science
B.V.