Istradefylline-13C,d3(Synonyms: KW-6002-13C,d3)

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Istradefylline-13C,d3 (Synonyms: KW-6002-13C,d3)

Istradefylline-13C,d3 是一种 13C- 和氘代标记的 Istradefylline。Istradefylline 是一种有效的，选择性的，可口服的 adenosine A2A receptor 拮抗剂，在帕金森疾病模型试验中，Ki 值为 2.2 nM。

Istradefylline-13C,d3(Synonyms: KW-6002-13C,d3)

Istradefylline-13C,d3 Chemical Structure

CAS No. : 2749234-46-4

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生物活性

Istradefylline-13C,d3 is the 13C- and deuterium labeled. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson’s disease.

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[86].

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

388.44

Formula

C1913CH21D3N4O4
CAS 号

2749234-46-4
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):211-223.

    [2]. Chen JF, et al. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson’s disease. J Neurosci. 2001 May 15;21(10):RC143.

    [3]. Shiozaki S, et al. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999 Nov;147(1):90-5.

    [4]. Kanda T, et al. Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Exp Neurol. 2000 Apr;162(2):321-7.

    [5]. Brambilla R, et al. Blockade of A2A adenosine receptors prevents basic fibroblast growth factor-induced reactive astrogliosis in rat striatal primary astrocytes. Glia. 2003 Aug;43(2):190-4.

    [6]. Mihara T, et al. Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinson’s disease and cognition. J Pharm

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