Ebastine-d₆  (Synonyms: 依巴斯汀-d₆; LAS-W 090-d₆; RP64305-d₆)

Ebastine-d₆ is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research^[1].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。

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

In rats, after intravenous administration of [¹⁴C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t_1/2 α) of 1.6 h and β-phase half-life (t_1/2 β) of 3.1 h^[4].
Following oral administration of [¹⁴C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (C_max) of 102 ng eq./ml at 2 h and decreased monophasically with t_1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with C_max of 1110 ng eq./ml at 4 h and with t_1/2 of 4.0 h^[4].

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

475.69

C₃₂H₃₃D₆NO₂

90729-43-4

依巴斯汀-d₆；艾巴斯啶-d₆

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]. Fu-Ming Tsai, et al. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503.  [Content Brief]

  [3]. J Sastre. Ebastine in allergic rhinitis and chronic idiopathic urticarial. Allergy. 2008 Dec;63 Suppl 89:1-20.  [Content Brief]

  [4]. Fujii, et al. Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats. Arzneimittelforschung. 1994 Apr;44(4):527-38.  [Content Brief]