Loratadine-d₄  (Synonyms: Loratidine-d₄; SCH 29851-d₄)

Loratadine-d₄ is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

386.91

C₂₂H₁₉D₄ClN₂O₂

381727-27-1

ClC1=CC=C(/C(C2=NC=CC=C2CC3)=C4CC([2H])([2H])N(C([2H])([2H])C/4)C(OCC)=O)C3=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Kay GG, Harris AG. Loratadine: a non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedation. Clin Exp Allergy. 1999 Jul;29 Suppl 3:147-50.;Menardo JL, Horak F, Danzig MR, Czarlewski W. A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4.;Monroe EW. Loratadine in the treatment of urticaria. Clin Ther. 1997 Mar-Apr;19(2):232-42.;Haria M, Fitton A, Peters DH. Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs. 1994 Oct;48(4):617-37.;Roman IJ, Danzig MR. Loratadine. A review of recent findings in pharmacology, pharmacokinetics, efficacy, and safety, with a look at its use in combination with pseudoephedrine. Clin Rev Allergy. 1993 Spring;11(1):89-110.;Shahen M, et al. Dengue virus causes changes of MicroRNA-genes regulatory network revealing potential targets for antiviral drugs. BMC Syst Biol. 2018 Jan 4;12(1):2.;Kleine-Tebbe J, et al. Inhibition of IgE- and non-IgE-mediated histamine release from human basophil leukocytes in vitro by a histamine H1-antagonist, desethoxycarbonyl-loratadine. J Allergy Clin Immunol. 1994;93(2):494-500.  [Content Brief]