Paliperidone-d₄ is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].

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].

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

430.51

C₂₃H₂₃D₄FN₄O₃

1020719-55-4

144598-75-4

固體

White to off-white

帕潘立酮 d₄

Room temperature in continental US; may vary elsewhere.

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

  [2]. Mauri MC, Paletta S, Maffini M, et al. Clinical pharmacology of atypical antipsychotics: an update. EXCLI J. 2014;13:1163-1191. Published 2014 Oct 13.  [Content Brief]

  [3]. Peng L, et al. Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3β signaling pathway. Schizophr Res. 2013 Jun;147(1):14-23.  [Content Brief]

  [4]. Yang MC, et al. Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Psychopharmacology (Berl). 2011 Oct;217(3):397-410.  [Content Brief]

  [5]. Kalman S, et al. 9-hydroxy-risperidone (9OHRIS) prevents stress-induced β-actin overexpression in rat hippocampus. Neuropsychopharmacol Hung. 2010 Sep;12(3):425-31.  [Content Brief]