Regadenoson-d3(Synonyms: CVT-3146-d3)

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Regadenoson-d3 (Synonyms: CVT-3146-d3)

Regadenoson-d3 (CVT-3146-d3) 是 Regadenoson 的氘代物。Regadenoson (CVT-3146) 是一种有效的选择性 A2A 腺苷受体激动剂,对大鼠和猪腺苷 A2A 受体的 Ki 分别为 290 和 1120 nM。Regadenoson 对 A2A 受体的选择性高于人 A1 和 A2B 受体,其选择性是 A1 受体的 13 倍。Regadenoson 是一种血管扩张剂,它改变了血管扩张剂心肌灌注显像的前景。Re

Regadenoson-d3(Synonyms: CVT-3146-d3)

Regadenoson-d3 Chemical Structure

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生物活性

Regadenoson-d3 (CVT-3146-d3) is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[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

393.37

Formula

C15H15D3N8O5

中文名称

瑞加德松 d3

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]. Jackson S, et al. The effect of regadenoson on the integrity of the human blood-brain barrier, a pilot study. J Neurooncol. 2017;132(3):513-519.

    [3]. Palle VP, et al. Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor. Bioorg Med Chem Lett. 2002;12(20):2935-2939.

    [4]. Golzar Y, et al. Regadenoson use in patients with chronic obstructive pulmonary disease: the state of current knowledge. Int J Chron Obstruct Pulmon Dis. 2014;9:129-137. Published 2014 Jan 22.

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