RAPID DISTRIBUTION OF TRYPTOPHOL (3-INDOLE ETHANOL) TO THE BRAIN AND OTHER TISSUES
RAPID DISTRIBUTION OF TRYPTOPHOL (3-INDOLE ETHANOL) TO THE BRAIN AND OTHER TISSUES
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DOI：
10.1172/jci109419
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发表时间：
1979-01-01
影响因子：
15.9
通讯作者：
MACINNIS, AJ
中科院分区：
文献类型：
--
作者：
CORNFORD, EM;BOCASH, WD;MACINNIS, AJ
色氨酸（3-吲哚乙醇）是一种诱导睡眠的化合物，在双硫仑治疗后在肝脏中形成，并在锥虫昏睡病中由寄生虫布氏冈比亚锥虫形成。制备、纯化和表征放射性标记的山梨醇，以确定其在动物中的组织分布。色氨酸具有高度亲脂性，辛醇：水分配系数为29.8。在颈动脉内注射[大鼠]后测定的脑提取物是高的（脑摄取指数= 117 . ±. 3.5%）和不饱和的，表明不存在载体系统。静脉注射给药后，乙醇在组织中的分布与相对血流量相关。当通过TLC分析时，静脉注射后2-5分钟，脑中残留的放射性超过85%与乙醇标准品共迁移。色氨酸显然与血清结合，并且在体内可以从血清白蛋白中剥离并在单个毛细血管转运中被脑摄取。在锥虫昏睡病或双硫仑治疗等状态下，远程形成的乙醇可能容易进入大脑（在单个毛细血管通道中100%清除），并可能导致嗜睡。
Tryptophol (3-indole ethanol) is a compound which induces sleep and is formed in the liver after disulfiram treatment and by the parasite Trypanosoma brucei gambiense in trypanosomal sleeping sickness. Radiolabeled tryptophol was prepared, purified and characterized for the purpose of defining its tissue distribution in animals. Tryptophol was highly lipophilic, with an octanol:water partition coefficient of 29.8. Brain extraction, determined after intracarotid injection [rats], was high (brain uptake index = 117 .+-. 3.5%) and nonsaturable, suggesting the absence of a carrier system. After i.v. administration, tryptophol distribution to tissues correlated with relative blood flow. More than 85% of the radioactivity remaining in brain 2-5 min after i.v. injection co-migrated with tryptophol standards when analyzed by TLC. Tryptophol apparently binds to serum and in vivo may be stripped from serum albumin and taken up by brain in a single capillary transit. In states such as trypanosomal sleeping sickness or disulfiram treatment, remotely formed tryptophol probably gains ready access to brain (it is 100% cleared in a single capillary passage) and may cause somnolence.