生物活性 | |||
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描述 | Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase with an IC50 of 7.82±0.12 μM. Allopurinol is almost completely metabolized to oxypurinol within two hours of oral administration [3]. Allopurinol is the most commonly used urate lowering therapy in the management of gout[4]. Allopurinol is generally well tolerated. The initial dosage of allopurinol should be low, particularly in patients with renal impairment. The dose should then be increased slowly until plasma concentrations of urate are sufficient to dissolve monosodium urate crystals (≤0.36 mmol/L)[5]. Along with preventing uric acid formation, allopurinol also has the ability to behave as a free radical scavenger of the superoxide anions and free radicals released during uric acid formation. Allopurinol has also been shown to decrease oxidative stress and ameliorate the morbidity and mortality of congestive heart failure patients by possibly improving mechano-energetic uncoupling, with the enhancement of myocardial contractility and the left ventricular ejection fraction[6]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
7.35mL 1.47mL 0.73mL |
36.73mL 7.35mL 3.67mL |
73.47mL 14.69mL 7.35mL |
参考文献 |
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