An antihistamine with antiserotonergic and anticholinergic activities
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Labeled Version(s)
29023Cyproheptadine-d3
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Cyproheptadine (hydrochloride hydrate)

Item No. 19551

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 mg

    $41

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    1 g

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    Product Description

    Cyproheptadine is an antihistamine with antiserotonergic and anticholinergic activities.1 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).2 Cyproheptadine reduces histamine-induced spasms in isolated guinea pig ileum (IC75 = 0.0014 μg/ml).3 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.4 Formulations containing cyproheptadine have been used in the treatment of allergic reactions including rhinitis, conjunctivitis, and urticaria.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Greaves, M.W. Antihistamines. Dermatol. Clin. 19(1), 53-62 (2001).

    2. Kakiuchi, M., Ohashi, T., Musoh, K., et al. Studies on the novel antiallergic agent HSR-609: Its penetration into the central nervous system in mice and guinea pigs and its selectivity for the histamine H1-receptor. Jpn. J. Pharmacol. 73(4), 291-298 (1997).

    3. Lish, P.M., Robbins, S.I., and Peters, E.L. Specificity of antihistamine drugs and involvement of the adrenergic system in histamine deaths in the guinea pig. J. Pharmacol. Exp. Ther. 153(3), 538-543 (1966).

    4. Takemoto, Y., Ito, A., Niwa, H., et al. Identification of cyproheptadine as an inhibitor of SET domain containing lysine methyltransferase 7/9 (Set7/9) that regulates estrogen-dependent transcription. J. Med. Chem. 59(8), 3650-3660 (2016).