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别嘌呤醇核糖苷

别嘌呤醇核糖苷用途

Allopurinol riboside是别嘌呤醇的代谢物,能有效地抑制寄生虫。

别嘌呤醇核糖苷名称

[ CAS 号 ]:
16220-07-8

[ 中文名 ]:
1-β-D-Ribofuranosyl-1H-pyrazolo[3,4-d]pyrimidine-4-one

[ 英文名 ]:
Allopurinol riboside

[英文别名 ]:

8-Aza-6-hydroxy-7-deazapurine riboside
Allopurinol ribonucleoside
8-AZA-7-DEAZAINOSINE
<4-Hydroxy-1H-pyrazolo<3,4-d>pyrimidin>-ribosid
Allopurinol-1-ribonucleoside

别嘌呤醇核糖苷生物活性

[ 描述 ]:

Allopurinol riboside是别嘌呤醇的代谢物,能有效地抑制寄生虫。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

天然产物 >> 糖和糖苷

[ 靶点 ]

Human Endogenous Metabolite

[体外研究]

别嘌呤醇-核糖苷竞争性抑制嘌呤核苷磷酸化酶对肌苷的作用,Ki为277μM。 PHA和Con A诱导的淋巴细胞胚细胞生成被别嘌呤醇-核糖苷以浓度依赖性方式显着抑制。当LPS用作促分裂原时,别嘌呤醇-核糖核苷酸淋巴细胞增殖的抑制作用不太明显。别嘌呤醇-核糖苷不能抑制体液免疫[1]。别嘌呤醇核糖苷是用于治疗利什曼病和美洲锥虫病的实验剂。别嘌呤醇核糖苷对寄生虫有效,因为一系列酶(类似于介导人类嘌呤挽救的酶)将其转化为4-氨基吡唑并嘧啶核糖核苷三磷酸,一种细胞毒性产物。别嘌呤醇核苷具有选择性毒性,因为它不会被人类相应的酶代谢[2]。

[体内研究]

施用后1.6小时,别嘌呤醇核糖苷在血浆中达到峰值,消除半衰期为3小时,稳态浓度在治疗范围内[3]。口服给药后,血浆中异丙肾上腺素核苷的意外低水平可归因于不完全吸收和快速肾清除。 Probenecid可降低别嘌呤醇核苷的肾清除率,延长血浆中别嘌呤醇核苷的半衰期,使血浆中别嘌呤醇核苷的含量增加三倍[4]。

[参考文献]

[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.

[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.

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

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

[相关活性小分子]

别嘌呤醇核糖苷物理化学性质

[ 密度 ]:
2.08g/cm3

[ 沸点 ]:
570.9ºC at 760mmHg

[ 分子式 ]:
C₁₀H₁₂N₄O₅

[ 分子量 ]:
268.22600

[ 闪点 ]:
299ºC

[ 精确质量 ]:
268.08100

[ PSA ]:
133.49000

[ 蒸汽压 ]:
3.62E-15mmHg at 25°C

[ 折射率 ]:
1.925

[ 储存条件 ]:
-20°C，密闭，干燥

别嘌呤醇核糖苷MSDS

详细MSDS(安全技术说明书)

别嘌呤醇核糖苷安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

别嘌呤醇核糖苷文献

Activity of inosine analogs against Pneumocystis carinii in culture.

Antimicrob. Agents Chemother. 30(1) , 181-3, (1986)

Three analogs of inosine, formycin B, allopurinol ribonucleoside, and 9-deazainosine, were tested for their ability to suppress proliferation of Pneumocystis carinii in culture with WI-38 cells. The o...

A tissue culture system for the growth of several species of Leishmania: growth kinetics and drug sensitivities.

Am. J. Trop. Med. Hyg. 38(2) , 304-7, (1988)

We have developed a simple in vitro method of infecting a continuous human macrophage cell line (U937) with promastigotes of several species of Leishmania. These include L. braziliensis braziliensis, ...

On the metabolism of allopurinol. Formation of allopurinol-1-riboside in purine nucleoside phosphorylase deficiency.

Biochem. Pharmacol. 32(14) , 2167-74, (1983)

Allopurinol-1-riboside, a major metabolite of allopurinol, is commonly thought to be directly synthesized by purine nucleoside phosphorylase (PNP) in vivo. As this enzyme is otherwise believed to func...

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