Iloperidone-d₃ hydrochloride  (Synonyms: 伊潘立酮盐酸盐-d₃)

Iloperidone-d₃ hydrochloride is deuterated labeled Iloperidone (HY-17410). Iloperidone (HP 873) is a D₂/5-HT₂ receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms^[1][2].

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.

Iloperidone is eliminated slowly, with a mean t_1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, t_max, or C_max. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events^[3].

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

465.96

C₂₄H₂₅D₃ClFN₂O₄

133454-47-4

伊潘立酮盐酸盐-d₃；哌啶酮-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 Feb;53(2):211-216.  [Content Brief]

  [2]. Kongsamut, S., et al., Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol, 1996. 317(2-3): p. 417-23.  [Content Brief]

  [3]. Sainati, S.M., et al., Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol, 1995. 35(7): p. 713-20.  [Content Brief]

  [4]. Albers, L.J., A. Musenga, and M.A. Raggi, Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market? Expert Opin Investig Drugs, 2008. 17(1): p. 61-75.  [Content Brief]