Allopurinol riboside

Research use only, not for human use.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.(In Vitro):Allopurinol riboside is effective against parasites including leishmaniasis and American trypanosomiasis. Allopurinol riboside is selectively toxic because it is not metabolized by the corresponding enzymes in humans. Humoral immunity is not suppressed by Allopurinol riboside. Lymphocyte blastogenesis induced by PHA and Con A is significantly suppressed by Allopurinol riboside in a concentration-dependent manner.(In Vivo):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. Allopurinol riboside peaks in plasma 1.6 hours after administration, has an elimination half-life of 3 h, and has steady-state concentrations in the therapeutic range.

Allopurinol-riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki 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. 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.

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. 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.

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Others

Other Targets

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16220-07-8

268.229

C10H12N4O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (372.81 mM)

OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1ncc2c1[nH]cnc2=O

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(-20℃)

With Ice Pack

≥ 2 years