Olopatadine-d₆ (hydrochloride)  (Synonyms: ALO4943A-d6 hydrochloride; KW4679-d6 hydrochloride)

Olopatadine-d₆ (ALO4943A-d₆; KW4679-d₆) hydrochloride is deuterium-labeled Olopatadine (hydrochloride) (HY-B0426A). Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4⁺ and CD8⁺ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis^[1][2][3].

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

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.

Isotopic labels can non-invasively track the distribution, transformation and clearance of compounds and their metabolites in the body through techniques such as mass spectrometry (MS) and nuclear magnetic resonance (NMR), which is beneficial to the study of pharmacometabolic kinetics (ADME).
Isotope labeling can reveal specific steps in metabolic pathways. Using compounds with stable isotope labels at specific locations directly in humans or animal models can also help verify drug mechanisms and evaluate unexpected side effects, improving the accuracy and efficiency of clinical research^[3].

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

379.91

C₂₁H₁₈D₆ClNO₃

140462-76-6

O=C(O)CC1=CC=C(C/2=C1)OC([2H])([2H])C3=C([2H])C([2H])=C([2H])C([2H])=C3C2=C\CCN(C)C.Cl

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 Feb;53(2):211-216.  [Content Brief]

  [2]. Baba A, et al. Olopatadine inhibits exocytosis in rat peritoneal mast cells by counteracting membrane surface deformation. Cell Physiol Biochem. 2015;35(1):386-396.  [Content Brief]

  [3]. Ito T, et al. Antihistaminic drug olopatadine downmodulates T cell chemotaxis toward CXCL10 by reducing CXCR3 expression, F-actin polymerization and calcium influx in patients with alopecia areata[J]. Journal of Dermatological Science, 2013, 72(1): 68-71.

  [4]. Murota H, et al. Olopatadine hydrochloride improves dermatitis score and inhibits scratch behavior in NC/Nga mice. Int Arch Allergy Immunol. 2010;153(2):121-132.  [Content Brief]