产品描述:
Desloratadine is a histamine H1 receptor antagonist (Ki = 0.97 nM) and an active metabolite of loratadine (Item No. 15625).{27482,64192} It is formed from loratadine primarily by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, and CYP2C19.{64193} 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.{64190} Desloratadine (10 mg/kg) reduces ovalbumin-induced sneezing, nose rubbing, eye watering, and congestion in ovalbumin-sensitized guinea pigs.{64191} It also increases the clearance of amyloid-β 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.{64190} Formulations containing desloratadine have been used in the treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria.