References of (E)-3-[6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-
yl]prop-2-enoic acid
Title: Acrivastine
CAS Registry Number: 87848-99-5
CAS Name: (2
E)-3-[6-[(1
E)-1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]-2-pyridinyl]-2-propenoic acid
Synonyms: (E)-6-[
(E)-3-(1-pyrrolidinyl)-1-
p-tolylpropenyl]-2-pyridineacrylic acid
Manufacturers' Codes: BW-270C; BW-825C; BW-A825C
Trademarks: Semprex (GSK)
Molecular Formula: C22H24N2O2
Molecular Weight: 348.44
Percent Composition: C 75.83%, H 6.94%, N 8.04%, O 9.18%
Literature 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). Evaluation of CNS effects: A. F. Cohen
et al., Clin. Pharmacol. Ther. 38, 381 (1985). Clinical trials in idiopathic urticaria: J. G. Gibson
et al., Dermatologica 169, 179 (1984); H. Neittaanmaki
et al., ibid. 177, 98 (1988); in allergic rhinitis: T. G. Gibbs
et al., J. Int. Med. Res. 16, 413 (1988). Review of pharmacology and therapeutic efficacy: R. N. Brogden, D. McTavish,
Drugs 41, 927-940 (1991).
Properties: Crystals from isopropanol, mp 222° (dec).
Melting point: mp 222° (dec)
NOTE: Combination with pseudoephedrine,
Duact (Glaxo Wellcome) .
Therap-Cat: Antihistaminic.
Keywords: Antihistaminic; Alkylamine Derivatives.