8225. Rimazolium Metilsulfate

Nomenclature

CAS number: 28610-84-6
3-(Ethoxycarbonyl)-6,7,8,9-tetrahydro-1,6-dimethyl-4-oxo-4H-pyrido[1,2-a]pyrimidinium methyl sulfate; 3-carboxy-6,7,8,9-tetrahydro-1,6-dimethyl-4-oxo-4H-pyrido[1,2-a]pyrimidinium methyl sulfate, ethyl ester; 1,6-dimethyl-3-carbethoxy-4-oxo-6,7,8,9-tetrahydrohomopyrimidazole methyl sulfate; MZ-144; MZ-0780; Ro-11-780; Probon (Chinoin).
C14H22N2O7S; mol wt 362.40.
C 46.40%, H 6.12%, N 7.73%, O 30.90%, S 8.85%.

Description and references

Prepn: Z. Mészáros et al., HU Teljes 519 (1970 to Chinoin), C.A. 74, 42374h (1971); eidem, Arzneim.-Forsch. 22, 815 (1972). Anti-inflammatory and analgesic effects in animals: K. Gyires et al., Drugs Exp. Clin. Res. 11, 493 (1985). Clinical analgesic effect: H. Graber, Int. J. Clin. Pharmacol. Ther. Toxicol. 6, 354 (1972); M. Haataja et al., Curr. Ther. Res. 22, 784 (1977). Series of articles on pharmacology, pharmacodynamics and toxicology: Arzneim.-Forsch. 21, 717-738 (1971). Toxicity data: J. Knoll et al., ibid. 719.

Chemical structure

Properties

White crystals, mp 165-166°. uv max: 336, 258 nm (ε 3630, 27500). Readily sol in water. LD50 in rats (mg/kg): 220 i.v.; 720 i.p.; 790 s.c.; 1600 orally (Knoll).

Therapeutic Category

Analgesic.