Cyproheptadine (hydrochloride hydrate)

Cyproheptadine is an antihistamine with antiserotonergic and anticholinergic activities. 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). Cyproheptadine reduces histamine-induced spasms in isolated guinea pig ileum (IC75 = 0.0014 µg/ml). 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 alpha (ERalpha) in MCF-7 cells. Formulations containing cyproheptadine have been used in the treatment of allergic reactions including rhinitis, conjunctivitis, and urticaria.Formal Name: 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-methyl-piperidine, monohydrochloride, sesquihydrate. CAS Number: 41354-29-4. Molecular Formula: C21H21N . HCl [1.5H2O]. Formula Weight: 350.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, Ethanol: 30 mg/mL, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/mL. lambdamax: 225, 287 nm. SMILES: CN(CC/1)CCC1=C2C(C=CC=C3)=C3C=CC4=C\2C=CC=C4.CN(CC/5)CCC5=C6C(C=CC=C7)=C7C=CC8=C\6C=CC=C8.Cl.O.O.O.Cl. InChi Code: InChI=1S/2C21H21N.2ClH.3H2O/c2*1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21,,,,,/h2*2-11H,12-15H2,1H3,2*1H,3*1H2. InChi Key: ZEAUHIZSRUAMQG-UHFFFAOYSA-N.