Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.

Allopurinol-riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a K_i of 277 μM. Lymphocyte blastogensis induced by PHA and Con A is significantly suppressed by allopurinol-riboside in a concentration-dependent manner. When LPS is used as a mitogen, the inhibition of allopurinol-ribosideon lymphocyte proliferation is less marked. Humoral immunity is not suppressed by allopurinol-riboside^[1]. Allopurinol riboside is an experimental agent for the treatment of leishmaniasis and American trypanosomiasis. Allopurinol riboside is effective against parasites, because a series of enzymes (analogous to those that mediate purine salvage in humans) convert it into 4-aminopyrazolopyrimidine ribonucleoside triphosphate, a cytotoxic product. Allopurinol riboside is selectively toxic, because it is not metabolized by the corresponding enzymes in humans^[2].

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

Allopurinol riboside peaks in plasma 1.6 hours after administration, has an elimination half-life of 3 hours, and steady-state concentrations in the therapeutic range^[3]. After oral administration, unexpectedly low levels of allopurinol riboside in plasma are attributable to incomplete absorption and rapid renal clearance. Probenecid reduces the renal clearance of allopurinol riboside, extends the half-life of allopurinol riboside in plasma, and triples the levels of allopurinol riboside in plasma^[4].

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

268.23

C₁₀H₁₂N₄O₅

16220-07-8

固体

White to off-white

别嘌呤醇核糖苷

• Alkaloids
• Indole Alkaloids

• 内源性代谢物

Room temperature in continental US; may vary elsewhere.

DMSO 中的溶解度 : 100 mg/mL (372.81 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

• 方案 一

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

  Solubility: ≥ 2.5 mg/mL (9.32 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

  生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

• 方案 二

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

  Solubility: ≥ 2.5 mg/mL (9.32 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

  20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

• 方案 三

  请依序添加每种溶剂： 10% DMSO    90% Corn Oil

  Solubility: ≥ 2.5 mg/mL (9.32 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Nishida Y, et al. Inhibition of purine nucleoside phosphorylase activity and of T-cell function with allopurinol-riboside. Agents Actions. 1979 Dec;9(5-6):549-52.  [Content Brief]

  [2]. Pacher P, et al. Therapeutic effects of xanthine oxidase inhibitors: renaissance half a century after the discovery of allopurinol. Pharmacol Rev. 2006 Mar;58(1):87-114.  [Content Brief]

  [3]. Shapiro TA, et al. Pharmacokinetics and metabolism of allopurinol riboside. Clin Pharmacol Ther. 1991 May;49(5):506-14.  [Content Brief]

  [4]. Were JB, et al. Effects of probenecid on the pharmacokinetics of allopurinol riboside. Antimicrob Agents Chemother. 1993 May;37(5):1193-6.  [Content Brief]