4928. Inaperisone

Nomenclature

CAS number: 99323-21-4
1-(4-Ethylphenyl)-2-methyl-3-(1-pyrrolidinyl)-1-propanone; (±)-4′-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone.
C16H23NO; mol wt 245.36.
C 78.32%, H 9.45%, N 5.71%, O 6.52%.

Description and references

Prepn: JP Kokai 84 33276; Y. Itho et al., US 4638009 (1984, 1987 both to Hokuriku). Pharmacology: K. Morikawa et al., Arzneim.-Forsch. 37, 331 (1987); idem et al., Eur. J. Pharmacol. 213, 409 (1992). Pharmacokinetics in rats: O. Nagata et al., Drug Metab. Dispos. 18, 902 (1990). GC/MS determn in human serum: idem et al., J. Chromatogr. 496, 456 (1989). Series of articles on toxicology: Yakuri to Chiryo 20, 1027-1115 (1992). Comparative clinical evaluation: K. Hiraga et al., Rinsho Yakuri 23, 635 (1992), C.A. 118, 247431y (1993).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 118230-97-0
HSR-770; HY-770; Riran (Yamanouchi).
C16H23NO.HCl; mol wt 281.82.
C 68.19%, H 8.58%, N 4.97%, O 5.68%, Cl 12.58%.

Properties

Colorless needles from methyl ethyl ketone (isolated as hydrate), mp 152-153°. Also reported as a white to yellowish white crystalline powder. Bitter taste. Very sol in water and methanol. LD50 orally in mice: 425 mg/kg (Itho).

Therapeutic Category

Muscle relaxant (skeletal).

Keywords

Muscle Relaxant (Skeletal)