An antihistamine with antiserotonergic and anticholinergic activities; binds to histamine H1

Cyproheptadine (hydrochloride hydrate) – 250 mg

Brand:
Cayman
CAS:
41354-29-4
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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.  

 

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Description

An antihistamine with antiserotonergic and anticholinergic activities; binds to histamine H1, muscarinic, and serotonin 5-HT2 receptors (Kis = 0.38, 1.26, and 0.83 nM, respectively, in radioligand binding assays); reduces histamine-induced spasms in isolated guinea pig ileum (IC75 = 0.0014 μg/ml); protects against intravenous histamine diphosphate-induced death (PD50 = 0.08 mg/kg) and delays induction of aerosolized histamine diphosphate-induced coughing (ED100sec = 0.29 mg/kg) in guinea pigs; inhibits the lysine methyltransferase SET7/9 (IC50 = 1 µM), decreasing the expression of estrogen receptor α (ERα) in MCF-7 cells

Formal name: 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-methyl-piperidine, monohydrochloride, sesquihydrate

Synonyms: 

Molecular weight: 350.9

CAS: 41354-29-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers||Research Area|Immunology & Inflammation|Allergy

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