Adiphenine-d4 hydrochloride(Synonyms: 盐酸阿地芬宁 d4 (盐酸盐))

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Adiphenine-d4 hydrochloride (Synonyms: 盐酸阿地芬宁 d4 (盐酸盐))

Adiphenine-d4 hydrochloride 是 Adiphenine hydrochloride 的氘代物。Adiphenine hydrochloride 是一种非竞争性的烟碱乙酰胆碱受体 (nAChR) 抑制剂，对 α1，α3β4，α4β2 和 α4β4 的 IC50 值分别为 1.9，1.8，3.7 和 6.3 µM。Adiphenine hydrochloride 具有抗惊厥作用。

Adiphenine-d4 hydrochloride(Synonyms: 盐酸阿地芬宁 d4 (盐酸盐))

Adiphenine-d4 hydrochloride Chemical Structure

CAS No. : 2468639-19-0

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生物活性

Adiphenine-d4 hydrochloride is the deuterium labeled Adiphenine hydrochloride. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects[1][2][3].

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

351.90

Formula

C20H22D4ClNO2
CAS 号

2468639-19-0
中文名称

盐酸阿地芬宁 d4 (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]. Spitzmaul, G., et al., The local anaesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms. Br J Pharmacol, 2009. 157(5): p. 804-17.

    [3]. Michelot, J., et al., Adiphenine plasma levels and blood-brain barrier crossing in the rat. Eur J Drug Metab Pharmacokinet, 1985. 10(4): p. 273-8.

    [4]. Gentry CL, et, al. Local anesthetics noncompetitively inhibit function of four distinct nicotinic acetylcholine receptor subtypes. J Pharmacol Exp Ther. 2001 Dec;299(3):1038-48.

    [5]. TANAKA K, et, al. Anticonvulsant properties of procaine, cocaine, adiphenine and related structures. Proc Soc Exp Biol Med. 1955 Oct;90(1):192-5.

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