Formulation: A solid
Formal Name: 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-(methyl-d3)-piperidine
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C21H18D3N
Formula Weight: 290,4
Shelf life (days): 1460
CAS Number: 2712455-05-3
Notes: Cyproheptadine-d3 is intended for use as an internal standard for the quantification of cyproheptadine (Item No. 19551) by GC- or LC-MS. Cyproheptadine is an antihistamine with antiserotonergic and anticholinergic activities.{42974} It binds to histamine H1, muscarinic, and serotonin 5-HT2 receptors (Kis = 0.38, 1.26, and 0.83 nM, respectively, in radioligand binding assays).{31530} Cyproheptadine reduces histamine-induced spasms in isolated guinea pig ileum (IC75 = 0.0014 μg/ml).{39804} It protects against intravenous histamine diphosphate-induced death with a 50% protective dose (PD50) value of 0.08 mg/kg and delays induction of aerosolized histamine diphosphate-induced coughing (ED100sec = 0.29 mg/kg) in guinea pigs. Cyproheptadine also inhibits the lysine methyltransferase SET7/9 (IC50 = 1 µM), decreasing the expression of estrogen receptor α (ERα) in MCF-7 cells.{31140} Formulations containing cyproheptadine have been used in the treatment of allergic reactions including rhinitis, conjunctivitis, and urticaria.