127. Acrivastine

Nomenclature

CAS number: 87848-99-5
(2E)-3-[6-[(1E)-1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propen-1-yl]-2-pyridinyl]-2-propenoic acid; (E)-6-[(E)-3-(1-pyrrolidinyl)-1-p-tolylpropenyl]-2-pyridineacrylic acid; BW-270C; BW-825C; BW-A825C; Semprex (GSK).
C22H24N2O2; mol wt 348.44.
C 75.83%, H 6.94%, N 8.04%, O 9.18%.

Description and references

Nonsedating type histamine H1-receptor antagonist; analog of triprolidine, q.v. Prepn: G. G. Coker, J. W. A. Findlay, EP 85959 (1983 to Wellcome); J. W. A. Findlay, G. G. Coker, US 4501893 (1985). Pharmacodynamics and pharmacokinetics in humans: A. F. Cohen et al., Eur. J. Clin. Pharmacol. 28, 197 (1985) DOI PubMed. Evaluation of CNS effects: A. F. Cohen et al., Clin. Pharmacol. Ther. 38, 381 (1985) PubMed. Clinical trials in idiopathic urticaria: J. G. Gibson et al., Dermatologica 169, 179 (1984) PubMed; H. Neittaanmaki et al., ibid. 177, 98 (1988) PubMed; in allergic rhinitis: T. G. Gibbs et al., J. Int. Med. Res. 16, 413 (1988) PubMed. Review of pharmacology and therapeutic efficacy: R. N. Brogden, D. McTavish, Drugs 41, 927-940 (1991) DOI PubMed.

Chemical structure

Properties

Crystals from isopropanol, mp 222° (dec).

Therapeutic Category

Antihistaminic.

Keywords

Antihistaminic; Alkylamine Derivatives