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时间:2021-05-16 17:28  编辑:wendj

产品名: Proxyphylline 修订日期: 6/30/2016产品说明书

化学性质

产品名:

Proxyphylline Cas No.:

603-00-9 分子量:

238.2 分子式:

C10H14N4O3 别名:

NSC 163343 化学名:

3,7-dihydro-7-(2-hydroxypropyl)-1,3-dimethyl-1H-purine-2,6-dione SMILES:

CN(C(N1C)=O)C2=C(N(CC(O)C)C=N2)C1=O 溶解性:

>10.1mg/mL in DMSO 储存条件:

Store at -20°C 一般建议: For obtaining a higher solubility , please warm the tube at 37°C

and shake it in the ultrasonic bath for a while.Stock solution can be

stored below -20°C for several months.

运输条件:

Evaluation sample solution : ship with blue ice

All other available size: ship with RT , or blue ice upon request

生物活性

靶点 :

GPCR/G protein 信号通路:

Adenosine Receptor 产品描述:

Ki: 82 nM for bovine brain A1 adenosine receptor

Proxyphylline is an A1 adenosine receptor antagonist.

The A1 adenosine receptor, the best characterized purinergic receptor family, can mediate responses via multiple pertussis toxin-sensitive GTP binding proteins to various different

effectors.

In vitro: Previous study showed that proxyphylline could selectively antagonize A1 adenosine

receptors versus A2 adenosine receptors (Ki = 850 μM for platelets) [1].

In vivo: In a previous study, rats that were allodynic following the vincristine injections were randomly allocated into four groups. Theoesberiven F (a combination of proxyphylline and Melilotus extract) was administered to rats. Results showed that the decreased paw withdrawal threshold induced by vincristine injection was increased by theoesberiven F treatment and the increased withdrawal frequency to cold stimuli was also reduced by theoesberiven F treatment [2].

Clinical trial: The proxyphylline PK was measured in healthy adults after intravenous, single oral and multiple oral doses to produce steady state. The mean peak time after oral administration was 29 min. The apparent volume of distribution was 0.611/kg. The ranges of biological half-life were 8.1-12.1 h and 8.3-12.6 h calculated from serum and urine data, respectively. In additioin, 24% of the dose was excreted in urine, which agreed with the relationship between the calculated total body clearance and the renal clearance of the drug [3].

参考文献:

[1] U. Schwabe, D. Ukena and M. J. Lohse. Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn-Schmiedeberg's Arch.Pharmacol. 330,212-221 (1985).

[2] S. Bang, Y. S. Kim and S. R. Jeong. Anti-allodynic effect of theoesberiven F in a

vincristine-induced neuropathy model. Exp. Ther. Med. 12(2), 799-803 (2016).

[3] Selvig K. Pharmacokinetics of proxyphylline in adults after intravenous and oral administration. Eur J Clin Pharmacol. 1981 Jan;19(2):149-55.

特别声明

产品仅用于研究,

不针对患者销售,望谅解。

每个产品具体的储存和使用信息显示在产品说明书中。ApexBio产品在推荐的条件下是稳定的。产品会根据不同的推荐温度进行运输。许多产品短期运输是稳定的,运输温度不同于长期储存的温度。我们确保我们的产品是在保持试剂质量的条件下运输的。收到产品后,按照产品说明书上的要求进行储存。

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