Desloratadine

Desloratadine is a histamine H1 receptor antagonist (Ki = 0.97 nM) and an active metabolite of loratadine (Cay-15625). It is formed from loratadine primarily by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, and CYP2C19. It inhibits calcium flow in neurons and glia in vitro (IC50s = 9.177 and 0.3185 µM, respectively), an effect that can be blocked by knockdown of the 5-HT receptor subtype 5-HT2A. Desloratadine (10 mg/kg) reduces ovalbumin-induced sneezing, nose rubbing, eye watering, and congestion in ovalbumin-sensitized guinea pigs. It also increases the clearance of amyloid-beta by microglia and reverses learning and memory deficits in the Morris water maze in the transgenic APP/PS1 mouse model of Alzheimer's disease when administered at a dose of 20 mg/kg per day. Formulations containing desloratadine have been used in the treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria.Formal Name: 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine. CAS Number: 100643-71-8. Synonyms: Descarboethoxyloratadine, NSC 675447, SCH 34117. Molecular Formula: C19H19ClN2. Formula Weight: 310.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 10 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 245 nm. SMILES: ClC1=CC(CCC2=C/3N=CC=C2)=C(C=C1)C3=C4CCNCC/4. InChi Code: InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2. InChi Key: JAUOIFJMECXRGI-UHFFFAOYSA-N.