中文名 | ALLOPURINOL RIBOSIDE |
英文名 | ALLOPURINOL RIBOSIDE |
别名 | 异胡芦巴核苷 别嘌呤醇核糖苷 化合物 T13539 ALLOPURINOL 核苷 |
英文别名 | 8-AZA-7-DEAZAINOSINE ALLOPURINOL RIBOSIDE Allopurinol ribonucleoside 1-BETA-D-RIBOFURANOSYLPYRAZOLO[3,4-D]PYRIMIDIN-4-ONE 1-β-d-ribofuranosyl-1h-pyrazolo[3,4-d]pyrimidine-4-one 1-BETA-D-RIBOFURANOSYL-1H-PYRAZOLO[3,4-D]PYRIMIDINE-4-ONE 1,5-Dihydro-1-β-D-ribofuranosyl-4H-pyrazolo[3,4-d]pyrimidin-4-one 1-[(2S,3S,4R,5R)-3,4,5,6-tetrahydroxyoxan-2-yl]-2H-pyrazolo[4,5-e]pyrimidin-4-one |
CAS | 16220-07-8 |
化学式 | C10H12N4O5 |
分子量 | 268.23 |
密度 | 2.08±0.1 g/cm3(Predicted) |
沸点 | 715.0±60.0 °C(Predicted) |
酸度系数 | 8.65±0.10(Predicted) |
存储条件 | 2-8°C |
体外研究 | 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. 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. |
体内研究 | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.728 ml | 18.641 ml | 37.282 ml |
5 mM | 0.746 ml | 3.728 ml | 7.456 ml |
10 mM | 0.373 ml | 1.864 ml | 3.728 ml |
5 mM | 0.075 ml | 0.373 ml | 0.746 ml |