2922. Desloratadine

Nomenclature

CAS number: 100643-71-8
8-Chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine; descarboethoxyloratadine; Sch-34117; Clarinex (Schering-Plough).
C19H19ClN2; mol wt 310.82.
C 73.42%, H 6.16%, Cl 11.41%, N 9.01%.

Description and 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); L. M. DuBuske, Expert Opin. Pharmacother. 6, 2511-2523 (2005).

Chemical structure

Properties

Crystals from hexane, mp 150-151°. Slightly sol in water; very sol in ethanol, propylene glycol.

Therapeutic Category

Antihistaminic.

Keywords

Antihistaminic; Tricyclics; Other Tricyclics