E-5-(2-溴乙烯基)-2'-脱氧尿苷在小鼠体内的药代动力学
Pharmacokinetics of E-5-(2-bromovinyl)-2'-deoxyuridine in mice.
作者信息
de Clercq E, Descamps J, de Somer P, Barr P J, Jones A S, Walker R T
出版信息
Antimicrob Agents Chemother. 1979 Aug;16(2):234-6. doi: 10.1128/AAC.16.2.234.
Abstract
The pharmacokinetics of the newly developed anti-herpes agent, E-5-(2-bromovinyl)-2'-deoxyuridine, was compared with that of the standard anti-herpes drug 5-iodo-2'-deoxyuridine. Both compounds were administered to mice at 100 mg/kg by either the intraperitoneal, subcutaneous, or oral route. The active blood drug levels achieved by E-5-(2-bromovinyl)-2'-deoxyuridine were considerably higher than those attained by 5-iodo-2'-deoxyuridine (serum peak concentrations: 40 to 100 and 4 to 10 mug/ml, respectively). Active blood drug levels could still be found 320 min after oral administration of E-5-(2-bromovinyl)-2'-deoxyuridine.
摘要
将新研发的抗疱疹药物E-5-(2-溴乙烯基)-2'-脱氧尿苷的药代动力学与标准抗疱疹药物5-碘-2'-脱氧尿苷进行了比较。两种化合物均通过腹腔内、皮下或口服途径以100mg/kg的剂量给予小鼠。E-5-(2-溴乙烯基)-2'-脱氧尿苷所达到的活性血药水平显著高于5-碘-2'-脱氧尿苷所达到的水平（血清峰值浓度分别为40至100μg/ml和4至10μg/ml）。口服E-5-(2-溴乙烯基)-2'-脱氧尿苷320分钟后仍可检测到活性血药水平。
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本文引用的文献
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Herpesvirus hominis infection in newborn mice. I. An experimental model and therapy with iododeoxyuridine.新生小鼠的人疱疹病毒感染。I. 一种实验模型及碘脱氧尿苷治疗法。
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(E)-5-(2-Bromovinyl)-2'-deoxyuridine: a potent and selective anti-herpes agent.（E）-5-（2-溴乙烯基）-2'-脱氧尿苷：一种高效且选择性的抗疱疹药物。
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9-(2-hydroxyethoxymethyl) guanine activity against viruses of the herpes group.9-（2-羟乙氧甲基）鸟嘌呤对疱疹病毒组病毒的活性。
Nature. 1978 Apr 13;272(5654):583-5. doi: 10.1038/272583a0.
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