Title: Desloratadine
CAS Registry Number: 100643-71-8
CAS Name: 8-Chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Additional Names: descarboethoxyloratadine
Manufacturers' Codes: Sch-34117
Trademarks: Clarinex (Schering-Plough)
Molecular Formula: C19H19ClN2
Molecular Weight: 310.82
Percent Composition: C 73.42%, H 6.16%, Cl 11.41%, N 9.01%
Literature References: Nonsedating-type histamine H1-receptor antagonist; active metabolite of loratadine, q.v. Also inhibits generation and release of inflammatory mediators from basophils and mast cells. Prepn: D. P. Schumacher et al., EP 208855; F. J. Villani, J. K. Wong, US 4659716 (both 1987 to Schering). GLC determn in plasma: R. Johnson et al., J. Chromatogr. B 657, 125 (1994). Pharmacology: W. Kreutner et al., Arzneim.-Forsch. 50, 345 (2000). Series of articles on clinical efficacy in rhinitis, asthma and urticaria: Allergy 56, Suppl. 65, 1-32 (2001). Review of pharmacology, pharmacokinetics and clinical efficacy: R. S. Geha, E. O. Meltzer, J. Allergy Clin. Immunol. 107, 751-762 (2001); D. K. Agrawal, Expert Opin. Invest. Drugs 10, 547-560 (2001).
Properties: Crystals from hexane, mp 150-151°. Slightly sol in water; very sol in ethanol, propylene glycol.
Melting point: mp 150-151°
Therap-Cat: Antihistaminic.
Keywords: Antihistaminic; Tricyclics; Other Tricyclics. |