| Bioactivity | Aripiprazole (1,1,2,2,3,3,4,4-d8) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM[1][2]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | Aripiprazole (1,1,2,2,3,3,4,4-d8) | ||||||||||||
| CAS | 1089115-04-7 | ||||||||||||
| Formula | C23H19D8Cl2N3O2 | ||||||||||||
| Molar Mass | 456.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Stip E, Tourjman V. et al. Aripiprazole in schizophrenia and schizoaffective disorder: A review. Clin Ther. 2010;32 Suppl 1:S3-20. [3]. Burris KD, Molski TF, Xu C et al. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther. 2002 Jul;302(1):381-9. [4]. Swainston Harrison T, Perry CM. Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [5]. Nagasaka Y, Oda K, Iwatsubo T, Kawamura A, Usui T.Nagasaka Y, Oda K, Iwatsubo T, Kawamura A, Usui T.Effects of aripiprazole and its active metabolite dehydroaripiprazole on the activities of drug efflux transporters expressed both in the intestine and at the blood-brain barrier.Biopharm Drug Dispos. 2012 Jul 27. doi: 10.1002/bdd.1801. |