Eperisone hydrochloride

Catalog No.S4877 Batch:S487701

Technical Data

Formula	C₁₇H₂₅NO.HCl
Molecular Weight	295.85	CAS No.	56839-43-1
Solubility (25°C)*	In vitro	DMSO	59 mg/mL (199.42 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description	Eperisone hydrochloride is muscle relaxant agent with antispasmodic effects. It is widely used in the treatment of patients with muscular contractures, low back pain or spasticity.
In vivo	Eperisone has very low bioavailability after oral administration in rats and extensively high oral clearance in humans. It undergoes extensive first-pass metabolism after oral administration in rats and humans because absorption of the drug is very high. The bioavailabilities in the intestine were 0.176 and 0.0879 at administration rates of 100 and 25 mg/h/kg, respectively, whereas those in the liver were 0.532 and 0.486, respectively. Eperisone has high metabolic clearance in the small intestine^[1].

Description

Eperisone hydrochloride is muscle relaxant agent with antispasmodic effects. It is widely used in the treatment of patients with muscular contractures, low back pain or spasticity.

In vivo

Eperisone has very low bioavailability after oral administration in rats and extensively high oral clearance in humans. It undergoes extensive first-pass metabolism after oral administration in rats and humans because absorption of the drug is very high. The bioavailabilities in the intestine were 0.176 and 0.0879 at administration rates of 100 and 25 mg/h/kg, respectively, whereas those in the liver were 0.532 and 0.486, respectively. Eperisone has high metabolic clearance in the small intestine^[1].

Protocol (from reference)

Animal Study:^{^[1]}	Animal Models Male Wistar rats Dosages 25 mg/h/kg Administration infused from the femoral vein, portal vein and duodenum

References

[1] Mihara K, et al. Pharm Res. 2001, 18(8):1131-7

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