An internal standard for the quantification of desloratadine
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Unlabeled Version(s)
16931Desloratadine
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Desloratadine-d4

Item No. 26776

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-chloro-6,11-dihydro-11-(4-piperidinylidene-3,3,5,5-d4)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
CAS Number
2713301-38-1
Synonyms
  • Descarboethoxyloratadine-d4
Molecular Formula
C19H15ClD4N2
Formula Weight
314.9
Purity
≥99% deuterated forms (d1-d4)
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 10 mg/mlEthanol: 30 mg/ml
SMILES
ClC1=CC(CCC2=C/3N=CC=C2)=C(C=C1)C3=C4C([2H])([2H])CNCC/4([2H])[2H]
InChi Code
InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2/i7D2,8D2
InChi Key
JAUOIFJMECXRGI-OSEHSPPNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $79

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    1 mg

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    5 mg

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    Product Description

    Desloratadine-d4 is intended for use as an internal standard for the quantification of desloratadine (Item No. 16931) by GC- or LC-MS. Desloratadine is a histamine H1 receptor antagonist (Ki = 0.97 nM) and an active metabolite of loratadine (Item No. 15625).1,2 It is formed from loratadine primarily by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, and CYP2C19.3 It also inhibits calcium flow in neurons and glia in vitro (IC50s = 9.177 and 0.3185 µM, respectively), an effect that can be blocked by knockdown of the 5-HT receptor subtype 5-HT2A.4 Desloratadine (10 mg/kg) reduces ovalbumin-induced sneezing, nose rubbing, eye watering, and congestion in ovalbumin-sensitized guinea pigs.5 It also increases the clearance of amyloid-β by microglia and reverses learning and memory deficits in the Morris water maze in the transgenic APP/PS1 mouse model of Alzheimer’s disease when administered at a dose of 20 mg/kg per day.4 Formulations containing desloratadine have been used in the treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lewis, T.A., Young, M.A., Arrington, M.P., et al. Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg. Med. Chem. Lett. 14(22), 5591-5594 (2004).

    2. Ramanathan, R., Alvarez, N., Su, A.-D., et al. Metabolism and excretion of loratadine in male and female mice, rats and monkeys. Xenobiotica 35(2), 155-189 (2005).

    3. Aratyn-Schaus, Y., and Ramanathan, R. Advances in high-resolution MS and hepatocyte models solve a long-standing metabolism challenge: The loratadine story. Bioanalysis 8(16), 1645-1662 (2016).

    4. Lu, J., Zhang, C., Lv, J., et al. Antiallergic drug desloratadine as a selective antagonist of 5HT2A receptor ameliorates pathology of Alzheimer’s disease model mice by improving microglial dysfunction. Aging Cell 20(1), e13286 (2021).

    5. Bahekar, P.C., Shah, J.H., Ayer, U.B., et al. Validation of guinea pig model of allergic rhinitis by oral and topical drugs. Int. Immunopharmacol. 8(11), 1540-1551 (2008).