13-06341. Muzolimine [Archived]

Nomenclature

CAS number: 55294-15-0
5-Amino-2-[1-(3,4-dichlorophenyl)ethyl]-2,4-dihydro-3H-pyrazol-3-one; 3-amino-1-(3,4-dichloro-α-methylbenzyl)-2-pyrazolin-5-one; Bayg 2821; Edrul (Bayer).
C11H11Cl2N3O; mol wt 272.13.
C 48.55%, H 4.07%, Cl 26.06%, N 15.44%, O 5.88%.

Description and references

High-ceiling loop diuretic. Prepn: E. Mller et al., DE 2319278; eidem, US 3957814 (1974, 1976 both to Bayer); eidem, Experientia 33, 382 (1977). In vitro effects: H. J. Kramer, Pharmatherapeutica 1, 353 (1977). Mechanism of action: M. Mussche, N. Lameire, Curr. Med. Res. Opin. 4, 462 (1977). Pharmacology: K. Meng et al., ibid. 555. Pharmacokinetics: O. Broers et al., Eur. J. Clin. Pharmacol. 15, 105 (1979); eidem, Curr. Med. Res. Opin. 6, 431 (1980). Use in advanced renal disease: A. D. Canton et al., Br. Med. J. 282, 595 (1981); P. Schmidt et al., Eur. J. Clin. Pharmacol. 20, 23 (1981). Toxicological studies: D. Lorke, P. Mürmann, Curr. Med. Res. Opin. 4, 716 (1977). Symposium on pharmacology, pharmacodynamics, toxicology, clinical studies: Clin. Nephrol. 19, Suppl. 1, S1-S117 (1983).

Chemical structure

Properties

Cryst from methanol, mp 127-129°. LD50 in mice, rats, dogs, rabbits (mg/kg): 1794, 1559, 2000, 1250 orally (Lorke, Mürmann).

Therapeutic Category

Diuretic; antihypertensive.

Keywords

Antihypertensive; Diuretic

Status

This monograph has been retired and is no longer subject to revision or update.