(R)-Baclofen-d4(Synonyms: Arbaclofen-d4; STX209-d4)

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(R)-Baclofen-d4 (Synonyms: Arbaclofen-d4; STX209-d4)

(R)-Baclofen-d4 (Arbaclofen-d4) 是 (R)-Baclofen 的氘代物。(R)-Baclofen (Arbaclofen) 是选择性 GABAB 受体激动剂。

(R)-Baclofen-d4(Synonyms: Arbaclofen-d4;  STX209-d4)

(R)-Baclofen-d4 Chemical Structure

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生物活性

(R)-Baclofen-d4 (Arbaclofen-d4)is the deuterium labeled (R)-Baclofen. (R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist[1].

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

217.69

Formula

C10H8D4ClNO2

中文名称

(R)-巴氯芬 d4

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]. Falch E, Hedegaard A, Nielsen L et al. Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations. J Neurochem. 1986 Sep;47(3):898-903.

    [3]. Hong YG, Henry JL. Effects of phaclofen and the enantiomers of baclofen on cardiovascular responses to intrathecal administration of L- and D-baclofen in the rat. Eur J Pharmacol. 1991 Apr 24;196(3):267-75.

    [4]. Orsnes G, Crone C, Krarup C et al. The effect of baclofen on the transmission in spinal pathways in spastic multiple sclerosis patients. Clin Neurophysiol. 2000 Aug;111(8):1372-9.

    [5]. Colombo G, Addolorato G, Agabio R et al. Role of GABA(B) receptor in alcohol dependence: reducing effect of baclofen on alcohol intake and alcohol motivational properties in rats and amelioration of alcohol withdrawal syndrome and alcohol craving in human alcoholics. Neurotox Res. 2004;6(5):403-14.

    [6]. Stetkarova I, Yablon SA, Kofler M, Stokic DS. Procedure- and device-related complications of intrathecal baclofen administration for management of adult muscle hypertonia: a review. Neurorehabil Neural Repair. 2010 Sep;24(7):609-19.

    [7]. Henderson C, et al. Reversal of disease-related pathologies in the fragile X mouse model by selective activation of GABAB receptors with arbaclofen. Sci Transl Med. 2012 Sep 19;4(152):152ra128.

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