Koster H, Halsema I, Scholtens E, Meerman J H, Pang K S, Mulder G J
Biochem Pharmacol. 1982 May 15;31(10):1919-24. doi: 10.1016/0006-2952(82)90498-1.
The pharmacokinetics of 2,6-dichloro-4-nitrophenol (DCNP) have been studied in the rat. Upon i.v. injection the plasma decay curve of DCNP showed a rapid distribution phase. After 30 min the plasma concentration reached a value that was constant for at least 90 min, indicating very slow elimination of DCNP. The volume of distribution was 88 ml/kg and a high degree of binding (over, 99%) of DCNP in vitro to bovine serum albumin was found. The concentration of DCNP in the liver was between 30 and 50% of the plasma values. While in vivo the effect of DCNP persisted for a long time, its action was readily reversible in the single-pass perfused rat liver. In vivo, the effect of the dose of DCNP on the inhibition of sulfation of the phenolic compound harmol was investigated. Upon the i.v. injection of 26 mumole DCNP/kg an instantaneous and complete inhibition of sulfation of harmol was found. Using this property of DCNP, the rate of sulfation of harmol in vivo was evaluated in relation to the dose and the time after injection of the substrate. Saturation of sulfation apparently occurred because the consumption of inorganic sulfate was extremely small.
已在大鼠中研究了2,6 - 二氯 - 4 - 硝基苯酚（DCNP）的药代动力学。静脉注射后，DCNP的血浆衰减曲线显示出快速分布相。30分钟后，血浆浓度达到一个至少90分钟保持恒定的值，表明DCNP的消除非常缓慢。分布容积为88 ml/kg，并且发现DCNP在体外与牛血清白蛋白具有高度结合（超过99%）。肝脏中DCNP的浓度为血浆值的30%至50%。虽然在体内DCNP的作用持续很长时间，但其作用在单通道灌注大鼠肝脏中很容易逆转。在体内，研究了DCNP剂量对酚类化合物哈尔满硫酸化抑制作用的影响。静脉注射26微摩尔DCNP/kg后，发现哈尔满硫酸化立即完全受到抑制。利用DCNP的这一特性，评估了体内哈尔满硫酸化速率与底物注射剂量和时间的关系。由于无机硫酸盐的消耗极少，硫酸化显然发生了饱和。
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