Title: Loratadine
CAS Registry Number: 79794-75-5
CAS Name: 4-(8-Chloro-5,6-dihydro-11
H-benzo[5,6]cyclohepta[1,2-
b]pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester
Synonyms: 11-[
N-(ethoxycarbonyl)-4-piperidylidene]-8-chloro-6,11-dihydro-5
H-benzo[5,6]cyclohepta[1,2-
b]pyridine
Manufacturers' Codes: Sch-29851
Trademarks: Alavert (Wyeth); Claritin (Schering-Plough); Clarityn (Schering-Plough); Clarytin (Schering-Plough); Lisino (Essex)
Molecular Formula: C22H23ClN2O2
Molecular Weight: 382.88
Percent Composition: C 69.01%, H 6.05%, Cl 9.26%, N 7.32%, O 8.36%
Literature References: Nonsedating-type histamine H1-receptor antagonist. Prepn: F. J. Villani,
US 4282233 (1981 to Schering); F. J. Villani
et al., Arzneim.-Forsch. 36, 1311 (1986). Pharmacology: A. Barnett
et al., Agents Actions 14, 590 (1984). Evaluation of CNS effects in humans: C. M. Bradley, A. N. Nicholson,
Eur. J. Clin. Pharmacol. 32, 419 (1987). Clinical pharmacokinetics: E. Radwanski
et al., J. Clin. Pharmacol. 27, 530 (1987). Clinical trial in allergic rhinitis: R. J. Dockhorn
et al., Ann. Allergy 58, 407 (1987); in comparison with terfenadine,
q.v.: F. Horak
et al., Arzneim.-Forsch. 38, 124 (1988); G. Bruttmann
et al., J. Allergy Clin. Immunol. 83, 411 (1989). HPLC determn in plasma: O. Q. P. Yin
et al., J. Chromatogr. B 796, 165 (2003). Review of pharmacology and therapeutic efficacy: M. Haria
et al., Drugs 48, 617-637 (1994).
Properties: Crystals from acetonitrile, mp 134-136°.
Melting point: mp 134-136°
Therap-Cat: Antihistaminic.
Keywords: Antihistaminic; Tricyclics; Other Tricyclics.