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Oxipurinol

奥昔嘌醇,别嘌呤二醇,羟嘌呤醇
Catalog No.
C3548
黄嘌呤氧化还原酶抑制剂
组合的产品项目
规格价格库存 数量
500mg
¥ 508.00
现货
1g
¥ 709.00
现货
5g
¥ 2,600.00
Ship with 10-15 days

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A

背景

Oxipurinol is a xanthine oxidoreductase inhibitor.

Xanthine oxidoreductase (XO), a complex molybdoflavoenzyme present in milk and many other tissues, has been studied for many years. XO is generally recognized as a critical enzyme in purine catabolism.

In vitro: Allopurinol could be rapidly oxidized by XO to its active metabolite oxypurinol (both isosteres of hypoxanthine and xanthine, respectively), which also could inhibit XO. Oxypurinol was identified as a noncompetitive inhibitor of XO; the formation of this compound was reported to be responsible for much of the pharmacological activity of allopurinol. Moreover, both allopurinol and oxypurinol showed free radical scavenging effects in isolated hearts, and exerted cardioprotective effects despite no detectable XO activities [1].

In vivo: Animal study found that in the vasculature of hypercholesterolemic rabbits, oxypurinol treatment led to a decrease in vascular free radical production [1].

Clinical trial: The PK parameters of oxypurinol in subjects with normal renal function were found to be t((1/2)) of 23.3 +/- 6.0 hours, CL/F of 0.31 +/- 0.07 mL/min/kg, V(d)/F of 0.59 +/- 0.16 L/kg, and renal clearance relative to creatinine clearance. Oxypurinol has been found to be cleared almost entirely by urinary excretion and, thus the dosage of allopurinol should be reduced in renal impairment [2].

References:
[1] P.  Pacher, A. Nivorozhkin and C. Szabó. Therapeutic effects of xanthine oxidase inhibitors: Renaissance half a century after the discovery of allopurinol. Pharmacological Reviews 58(1), 87-114 (2006).
[2] Day RO, Graham GG, Hicks M, McLachlan AJ, Stocker SL, Williams KM.  Clinical pharmacokinetics and pharmacodynamics of allopurinol and oxypurinol. Clin Pharmacokinet. 2007;46(8):623-44.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt152.1
Cas No.2465-59-0
FormulaC5H4N4O2
SynonymsAlloxanthine|NSC 76239
Solubilityinsoluble in EtOH; insoluble in H2O; ≥5.16 mg/mL in DMSO with ultrasonic
Chemical Name1H-​pyrazolo[3,​4-​d]​pyrimidine-​4,​6(5H,​7H)​-​dione
SDFDownload SDF
Canonical SMILESO=C1C2=C(NN=C2)NC(N1)=O
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