Astemizole-d₃  (Synonyms: 阿司咪唑-d₃)

Astemizole-d₃ is the deuterium labeled Astemizole. Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects^[1][2].

氢、碳和其他元素的稳定重同位素已被掺入药物分子中，主要用作药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注。

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

461.59

阿司咪唑-d₃

C₂₈H₂₈D₃FN₄O

1189961-39-4

68844-79-9

阿司咪唑-d₃

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]. Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21(2):294-300.  [Content Brief]

  [3]. Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61.  [Content Brief]