A P2X7 receptor antagonist, an antispasmodic agent, and a muscle relaxant
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Eperisone

Item No. 46311

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(4-ethylphenyl)-2-methyl-3-(1-piperidinyl)-1-propanone, monohydrochloride
CAS Number
64840-90-0
Synonyms
  • E-0646
Molecular Formula
C17H25NO
Formula Weight
259.4
Purity
≥98%
Formulation (Request formulation change)
A neat oil
SMILES
O=C(C(CN1CCCCC1)C)C2=CC=C(CC)C=C2
InChi Code
InChI=1S/C17H25NO/c1-3-15-7-9-16(10-8-15)17(19)14(2)13-18-11-5-4-6-12-18/h7-10,14H,3-6,11-13H2,1-2H3
InChi Key
SQUNAWUMZGQQJD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

    $37

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    50 mg

    $70

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    Product Description

    Eperisone is an antagonist of the purinergic P2X7 receptor (IC50 = 12.59 nM for the human receptor), an antispasmodic agent, and a muscle relaxant.1,2,3 It is selective for the P2X7 receptor over the P2X1-5 receptors (IC50s = >10,000, >10,000, 7,158, >10,000, and >10,000 nM, respectively).1 Eperisone also inhibits step depolarization-evoked peak sodium currents in a whole-cell patch-clamp assay using dorsal root ganglion (DRG) neurons (IC50 = 250 µM) and step depolarization-evoked calcium currents by 36% in a whole-cell patch-clamp assay using DRG neurons at 320 µM.3 It reduces contractions induced by potassium or serotonin (5-HT; Item No. 14332) in guinea pig basilar artery rings at 10 and 50 µM.2 Eperisone (10 mg/kg) inhibits dorsal root stimulation-induced ventral root reflexes in spinal rats.3 It also decreases collagen levels and total and tissue elastance and increases forced vital capacity in a mouse model of pulmonary fibrosis.4 Formulations containing eperisone have been used in the treatment of cervical syndrome, shoulder periarthritis, low back pain, and spastic paralysis but have been associated with immediate hypersensitivity and anaphylaxis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Okada, M., and Nose, T. Eperisone hydrochloride, a muscle relaxant, is a potent P2X7 receptor antagonist. Chem. Pharm. Bull. (Tokyo) 72(3), 345-348 (2024).

    2. Fujioka, M., and Kuriyama, H. Eperisone, an antispastic agent, possesses vasodilating actions on the guinea-pig basilar artery. J. Pharmacol. Exp. Ther. 235(3), 757-763 (1985).

    3. Kocsis, P., Farkas, S., Fodor, L., et al. Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels. J. Pharmacol. Exp. Ther. 315(3), 1237-1246 (2005).

    4. Tanaka, K.I., Shimoda, M., Sugizaki, T., et al. Therapeutic effects of eperisone on pulmonary fibrosis via preferential suppression of fibroblast activity. Cell Death Discov. 8(1), 52 (2022).