A histamine H1 receptor antagonist
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Labeled Version(s)
34246Carbinoxamine-d6 (maleate)
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Carbinoxamine (maleate)

Item No. 23937

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(4-chlorophenyl)-2-pyridinylmethoxy]-N,N-dimethyl-ethanamine, (2Z)-2-butenedioate
CAS Number
3505-38-2
Synonyms
  • NSC 62362
Molecular Formula
C16H19ClN2O • C4H4O4
Formula Weight
406.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Chloroform: Slightly SolubleMethanol: Slightly Soluble
SMILES
CN(C)CCOC(C1=CC=C(Cl)C=C1)C2=CC=CC=N2.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C16H19ClN2O.C4H4O4/c1-19(2)11-12-20-16(15-5-3-4-10-18-15)13-6-8-14(17)9-7-13;5-3(6)1-2-4(7)8/h3-10,16H,11-12H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
InChi Key
GVNWHCVWDRNXAZ-BTJKTKAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 g

    $31

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    5 g

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    10 g

    $157

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    Product Description

    Carbinoxamine is a competitive histamine H1 receptor antagonist (Ki = 2.3 nM) and first generation antihistamine.1 It also competes with [3H]diltiazem, an L-type calcium channel blocker, for binding to the benzothiazepine site on rat cardiomyocytes (Ki = 1.08 nM).2 Carbinoxamine decreases negative inotropic activity in isolated guinea pig left atria by 76% (EC50 = 250 nM) and negative chronotropic activity in guinea pig spontaneously beating isolated right atria (EC50s = 250 and 480 nM, respectively) by 48% compared with control. Formulations containing carbinoxamine have been used in the treatment of allergic rhinitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tran, V.T., Chang, R.S.L., and Snyder, S.H. Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramine. Proc. Natl. Acad. Sci. USA 75(12), 6290-6294 (1978).

    2. Carosati, E., Budriesi, R., Ioan, P., et al. Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening. J. Med. Chem. 51(18), 5552-5565 (2008).