394. Amezinium Methyl Sulfate

Nomenclature

CAS number: 30578-37-1
4-Amino-6-methoxy-1-phenylpyridazinium methyl sulfate (1:1); LU-1631; Regulton (Knoll); Risumic (Dainippon); Supratonin (Grünenthal).
C12H15N3O5S; mol wt 313.33.
C 46.00%, H 4.83%, N 13.41%, O 25.53%, S 10.23%.

Description and references

Sympathomimetic agent with vascular and cardiac activity. Prepn: F. Richenender, R. Kropp, DE 1912941; eidem, US 3631038 (1970, 1971 both to BASF). Series of articles on synthesis, pharmacology, mechanism of action, metabolism, pharmacokinetics, bioavailability, clinical trials: Arzneim.-Forsch. 31, 1527-1671 (1981). Acute toxicity data: H. J. Teschendorf, ibid. 1580. HPLC determn in human plasma: D. Hotz, E. Brode, J. Chromatogr. 277, 217 (1983). Disposition and identification of major metabolites in rats: K. Nambu et al., Arzneim.-Forsch. 38, 909 (1988).

Chemical structure

Properties

Crystals from water, mp 176° (dec). LD50 in mice, rats (mg/kg): 1630, 1410 orally; 40.4, 45.5 i.v. (Teschendorf).

Therapeutic Category

Antihypotensive.

Keywords

Antihypotensive