A histamine H1 receptor antagonist
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Cyclizine (hydrochloride)

Item No. 31190

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(diphenylmethyl)-4-methyl-piperazine, monohydrochloride
CAS Number
303-25-3
Molecular Formula
C18H22N2 • HCl
Formula Weight
302.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: 1 mg/ml
SMILES
CN1CCN(C(C2=CC=CC=C2)C3=CC=CC=C3)CC1.Cl
InChi Code
InChI=1S/C18H22N2.ClH/c1-19-12-14-20(15-13-19)18(16-8-4-2-5-9-16)17-10-6-3-7-11-17;/h2-11,18H,12-15H2,1H3;1H
InChi Key
UKPBEPCQTDRZSE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    250 mg

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    Cayman Chemical
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    Product Description

    Cyclizine is a histamine H1 receptor antagonist.1,2,3 It binds selectively to histamine H1 receptors (Kd = 5 nM) over H2 and H3 receptors (Kds = 1,600 and >580 nM, respectively).3 Cyclizine inhibits anti-IgE-induced histamine release from isolated human lung fragments with an IC50 value of 5.42 µM but induces histamine release with a 50% release concentration (RC50) of 10.81 µM.4 It reduces LPS-induced nitrite accumulation and protein levels of induced nitric oxide synthase (iNOS) in RAW 264.7 cells when used at a concentration of 100 nM.2 Cyclizine (10 and 20 mg/kg) reduces immobility in the forced swim test in rats.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hamlin, K.E., Weston, A.W., Fischer, F.E., et al. Histamine antagonists. II.1 Unsymmetrical 1,4-disubstituted piperazines. J. Am. Chem. Soc. 71(8), 2731-2734 (2019).

    2. Králová, J., Račková, L., Pekarová, M., et al. The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicity. Int. Immunopharmacol. 9(7-8), 990-995 (2009).

    3. Hill, S.J. Distribution, properties, and functional characteristics of three classes of histamine receptor. Pharmacol. Rev. 42(1), 45-83 (1990).

    4. Church, M.K., and Gradidge, C.F. Inhibition of histamine release from human lung in vitro by antihistamines and related drugs. Br. J. Pharmacol. 69(4), 663-667 (2019).

    5. Khanwelkar, C.C., Gokhale, D.V., Santakke, A.V., et al. Effects of H1–receptor antagonists in antidepressant tests in rats. Al Ameen J. Med. Sci. 1(2), 84-92 (2008).