111. Acipimox

Nomenclature

CAS number: 51037-30-0
5-Methyl-2-pyrazinecarboxylic acid 4-oxide; 2-carboxy-5-methylpyrazine 4-oxide; K-9321; Olbemox (Pharmacia); Olbetam (Pharmacia).
C6H6N2O3; mol wt 154.12.
C 46.76%, H 3.92%, N 18.18%, O 31.14%.

Description and references

Prepn: V. Ambrogi et al., DE 2319834; eidem, US 4002750 (1973, 1977 both to Carlo Erba). Prepn and toxicology: eidem, Eur. J. Med. Chem. 15, 157 (1980). Pharmacological profile: P. P. Lovisolo et al., Pharmacol. Res. Commun. 13, 151, 163 (1981) DOI PubMed. Pharmacokinetics: L. M. Fuccella et al., Clin. Pharmacol. Ther. 28, 790 (1980) PubMed; L. Musatti et al., J. Int. Med. Res. 9, 381 (1981) PubMed. Mechanism of action: K. Aktories et al., Arzneim.-Forsch. 33, 1525 (1983).

Chemical structure

Properties

Crystals from water, mp 177-180°. LD50 orally in mice: 3500 mg/kg (Ambrogi).

Therapeutic Category

Antilipemic.

Keywords

Antilipemic; Nicotinic Acid Derivatives