A histamine H1 receptor inverse agonist
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Loratadine

Item No. 15625

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid, ethyl ester
CAS Number
79794-75-5
Synonyms
  • SCH 29851
Molecular Formula
C22H23ClN2O2
Formula Weight
382.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
247 nm
SMILES
ClC(C=C1)=CC(CCC2=C/3N=CC=C2)=C1C3=C4CCN(C(OCC)=O)CC/4
InChi Code
InChI=1S/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5-6,9-10,12-13H2,1H3
InChi Key
JCCNYMKQOSZNPW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    Loratadine is a non-sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H1 receptors (Ki = 35 nM).1,2,3 It has been shown to inhibit the release of leukotriene C4 (IC50 = 8 µM) and histamine (IC50 = 11 µM) from rodent mast cells and to inhibit allergic bronchospasm in guinea pigs with an ED50 value of 0.40 mg/kg.4 Formulations containing loratadine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ahn, H.S., and Barnett, A. Selective displacement of [3H]mepyramine from peripheral vs. central nervous system receptors by loratadine, a non-sedating antihistamine. Eur. J. Pharmacol. 127(1-2), 153-155 (1986).

    2. Kay, G.G., and Harris, A.G. Loratadine: A non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedation. Clin. Exp. Allergy 29(Suppl 3), 147-150 (1999).

    3. Barnett, A., Iorio, L.C., Kreutner, W., et al. Evaluation of the CNS properties of SCH 29851, a potential non-sedating antihistamine. Agents Actions 43(3-4), 149-156 (1994).

    4. Kreutner, W., Chapman, R.W., Gulbenkian, A., et al. Antiallergic activity of loratadine, a non-sedating antihistamine. Allergy 42(1), 57-63 (1987).