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Chemical Compound Review

Eperisona     1-(4-ethylphenyl)-2-methyl-3- (1...

Synonyms: eperisone, Eperisonum, EMPP, SureCN194769, CHEMBL1902981, ...
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Disease relevance of eperisone


High impact information on eperisone


Biological context of eperisone

  • In vitro, (+)-3-(3-[3H]hydroxyphenyl)-N-(1-propylpiperidine) ((+)-[3H]3-PPP) specific binding, in rat brain membrane, was prevented by eperisone and the IC50 value was 0.43 nM [6].
  • These results suggest that eperisone predominantly inhibits synaptic transmission of the MVN ascending neurons [7].
  • Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone [8].
  • The cross-correlation analysis suggested that the membrane potentials of both tonic and phasic motoneurons are equally lowered by eperisone or that monosynaptic transmission from primary afferents of muscle spindles to motoneurons is inhibited by eperisone [9].
  • The safety analysis showed persistent vomiting (n=1), fatigue (n=1), headache and dry mouth (n=2), epigastric pain (n=1) and slight changes in blood pressure under Eperisone which was generally well tolerated by the patients [10].

Anatomical context of eperisone

  • Eperisone was biotransformed to HMO by rat intestinal microsomes, and this was inhibited by alpha-naphthoflavone and an anti-rat CYP1A antibody [5].
  • CONCLUSIONS: Those data strongly suggest that eperisone may be metabolized to HMO by CYP1A in rat intestinal microsomes during the first-pass through the epithelium of the small intestine [5].
  • Effects of eperisone, an antispasmodic in skeletal muscle, were investigated in helical strips of dog saphenous artery and vein [11].
  • Effects of eperisone applied by microiontophoresis on neurons in the medial and lateral vestibular nuclei [7].
  • In addition, iontophoretically applied eperisone in doses of 50-100 nA inhibited the orthodromic spike elicited by vestibular nerve stimulation in the MVN monosynaptic neurons projecting to the abducens nucleus (ascending neuron), without affecting that in the MVN neurons projecting to the spinal cord (descending neuron) [7].

Associations of eperisone with other chemical compounds


Gene context of eperisone

  • Eperisone is determined using ESI in a single-quadrupole MS [17].

Analytical, diagnostic and therapeutic context of eperisone

  • In contrast, intravenous injection of eperisone produced either a rapidly reversible depression of responses to both noxious and innocuous stimuli or had no effect on these responses [3].
  • In the intestinal perfusion experiment, the appearance clearance to the portal vein from the intestinal lumen was much lower than the elimination clearance from the intestinal lumen, resulting in high metabolic clearance of eperisone in the small intestine [5].
  • Treatment with eperisone (10(-5) M) potentiated the contractile response to electrical stimulation of adrenergic nerves; the potentiating effect was suppressed by yohimbine [11].


  1. Muscle cramps in chronic liver diseases and treatment with antispastic agent (eperisone hydrochloride). Kobayashi, Y., Kawasaki, T., Yoshimi, T., Nakajima, T., Kanai, K. Dig. Dis. Sci. (1992) [Pubmed]
  2. The efficacy and safety of eperisone in patients with cervical spondylosis: results of a randomized, double-blind, placebo-controlled trial. Bose, K. Methods and findings in experimental and clinical pharmacology. (1999) [Pubmed]
  3. Effects of tizanidine, eperisone and afloqualone on feline dorsal horn neuronal responses to peripheral cutaneous noxious and innocuous stimuli. Davies, J. Neuropharmacology (1989) [Pubmed]
  4. Eperisone, an antispastic agent, possesses vasodilating actions on the guinea-pig basilar artery. Fujioka, M., Kuriyama, H. J. Pharmacol. Exp. Ther. (1985) [Pubmed]
  5. Intestinal first-pass metabolism of eperisone in the rat. Mihara, K., Matsumura, M., Yoshioka, E., Hanada, K., Nakasa, H., Ohmori, S., Kitada, M., Ogata, H. Pharm. Res. (2001) [Pubmed]
  6. Sigma receptor modulation of the muscle relaxant action of eperisone. Hasegawa, Y., Kaku, S., Araki, H., Otomo, S. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. (1992) [Pubmed]
  7. Effects of eperisone applied by microiontophoresis on neurons in the medial and lateral vestibular nuclei. Noma, S., Sasa, M., Ohno, Y., Matsuoka, I., Takaori, S. Jpn. J. Pharmacol. (1986) [Pubmed]
  8. Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone. Yang, S.I., Park, H.Y., Lee, S.H., Lee, S.J., Han, O.Y., Lim, S.C., Jang, C.G., Lee, W.S., Shin, Y.H., Kim, J.J., Lee, S.Y. Pharmacology (2004) [Pubmed]
  9. Effects of eperisone-HCl on the stretch reflex in anesthetized cats. Nakajima, Y., Wada, N. Jpn. J. Pharmacol. (1989) [Pubmed]
  10. Eperisone compared to physiotherapy on muscular tone of stroke patients: a prospective randomized open study. Tariq, M., Akhtar, N., Ali, M., Rao, S., Badshah, M., Irshad, M. JPMA. The Journal of the Pakistan Medical Association. (2005) [Pubmed]
  11. Mechanisms of action of eperisone on isolated dog saphenous arteries and veins. Inoue, S., Bian, K., Okamura, T., Okunishi, H., Toda, N. Jpn. J. Pharmacol. (1989) [Pubmed]
  12. Long-lasting muscle relaxant activity of eperisone hydrochloride after percutaneous administration in rats. Matsunaga, M., Uemura, Y., Yonemoto, Y., Kanai, K., Etoh, H., Tanaka, S., Atsuta, Y., Nishizawa, Y., Yamanishi, Y. Jpn. J. Pharmacol. (1997) [Pubmed]
  13. Anti-nicotinic and anti-muscarinic actions of eperisone in the isolated canine atrium. Saegusa, K., Furukawa, Y., Akahane, K., Haniuda, M., Chiba, S. Jpn. J. Pharmacol. (1991) [Pubmed]
  14. Effect of a centrally-acting muscle relaxant, eperisone hydrochloride, on muscle sympathetic nerve activity in humans. Iwase, S., Mano, T., Saito, M., Ishida, G. Funct. Neurol. (1992) [Pubmed]
  15. In vivo and in vitro evidence for a common carrier mediated transport of choline and basic drugs through the blood-brain barrier. Kang, Y.S., Terasaki, T., Ohnishi, T., Tsuji, A. J. Pharmacobio-dyn. (1990) [Pubmed]
  16. Antinociceptive effects of sodium channel-blocking agents on acute pain in mice. Sakaue, A., Honda, M., Tanabe, M., Ono, H. J. Pharmacol. Sci. (2004) [Pubmed]
  17. Rapid and sensitive liquid chromatography-electrospray ionization-mass spectrometry method for the determination of eperisone in human plasma: method and clinical applications. Ding, L., Wei, X., Zhang, S., Sheng, J., Zhang, Y. Journal of chromatographic science. (2004) [Pubmed]
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