Cariprazine-d6 hydrochloride(Synonyms: RGH188-d6 hydrochloride)

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Cariprazine-d6 hydrochloride (Synonyms: RGH188-d6 hydrochloride)

Cariprazine-d6 (RGH188-d6) hydrochloride 是 Cariprazine hydrochloride 的氘代物。Cariprazine hydrochloride 是一种新型抗精神病候选药物，结合D3, D2 和 5-HT1A 的 Ki 为0.085 nM，0.49 nM，2.6 nM。

Cariprazine-d6 hydrochloride(Synonyms: RGH188-d6 hydrochloride)

Cariprazine-d6 hydrochloride Chemical Structure

CAS No. : 2714418-94-5

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生物活性

Cariprazine-d6 (RGH188-d6) hydrochloride is the deuterium labeled Cariprazine hydrochloride. Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

469.91

Formula

C21H27D6Cl3N4O
CAS 号

2714418-94-5
中文名称

卡利拉嗪 d6 (盐酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

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

    [2]. Seneca N, et al. Occupancy of dopamine D2 and D3 and serotonin 5-HT1A receptors by the novel antipsychotic drug candidate, cariprazine (RGH-188), in monkey brain measured using positron emission tomography. Psychopharmacology (Berl). 2011 Dec;218(3):579-8

    [3]. Kiss B, et al. Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile. J Pharmacol Exp Ther. 2010 Apr;333(1):328-40.

    [4]. Zimnisky R, et al. Cariprazine, a dopamine D(3)-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse. Psychopharmacology (Berl). 2013 Mar;226(1):91-100

    [5]. Gao Y, et al. Cariprazine exerts antimanic properties and interferes with dopamine D2 receptor β-arrestin interactions. Pharmacol Res Perspect. 2015 Feb;3(1):e00073.

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