9705. Trimetazidine

Nomenclature

CAS number: 5011-34-7
1-[(2,3,4-Trimethoxyphenyl)methyl]piperazine.
C14H22N2O3; mol wt 266.34.
C 63.13%, H 8.33%, N 10.52%, O 18.02%.

Description and references

Coronary vasodilator. Prepn: Regnier, Canevari, FR 1302958 (1962 to Sci. Union et Cie, Soc. Fran. Rech. Med.); FR M805; J. Servier, US 3262852 (1961, 1966 to Biofarma). Pharmacology: Fujita, Jpn. J. Pharmacol. 17, 19 (1967); Nagata et al., ibid. 19, 628 (1969); 21, 337 (1971). GC-MS determn in biological fluids: L. Fay et al., J. Chromatogr. 490, 198 (1989). Review of pharmacology, toxicology and clinical studies: C. Harpey et al., Cardiovasc. Drug Rev. 6, 292-312 (1989).

Chemical structure

Properties

bp2 200-205°.

Derivative

Dihydrochloride.

Nomenclature

CAS number: 13171-25-0
Kyurinett (Zensei); Vastarel F (Kyoto); Yoshimilon (Kowa Yakuhin).
C14H22N2O3.2HCl; mol wt 339.26.
C 49.56%, H 7.13%, N 8.26%, O 14.15%, Cl 20.90%.

Properties

Crystals, mp 225-228°. LD50 in male, female mice, rats (mg/kg): 91, 107, 124, 124 i.v.; 264, 245, 327, 288 i.p.; 528, 608, 1147, 987 orally (Harpey).

Therapeutic Category

Antianginal.

Keywords

Vasodilator (Coronary)