N-Methyl-beta-carboline-3-carboxamide (FG7142), an anxiogenic agent in the environment and evaluation of its exposure level in humans

FG 7142 （n -甲基- β -carboline-3-carboxamide）是一种焦虑剂，用于研究人类焦虑的发病机制。FG 7142被归类为苯二氮卓类受体的部分逆激动剂，不仅在实验动物中产生强烈的焦虑样综合征，在人类中也会产生严重的焦虑。本项目重点研究FG - 7142在环境中的分布、形成机制以及环境中FG - 7142对人体的影响。(1)用高效液相色谱法测定了卷烟烟雾、空气颗粒物、汽车尾气颗粒物、焚化炉灰、树叶的烟气冷凝物和室内空气中的卷烟烟雾中FG 7142的含量。这种化合物在香烟烟雾、空气中的颗粒物、树叶的烟雾凝结物和被香烟烟雾污染的室内空气中检测到，但在汽车尾气颗粒物、香烟和树叶本身中没有检测到。这些发现表明fg7142在环境中广泛分布，fg7142可能是通过植物燃烧形成的。(2)自动抽烟机采集的木屑烟凝结液中检测到FG 7142。然而，这种化合物尚未在木屑本身的二氯甲烷提取物中检测到。此外，烟气冷凝液中FG 7142的产率随色氨酸和含有羧酸酯部分的β -碳胺的添加量的增加而呈剂量依赖性增加。这些发现表明，FG 7142是在植物燃烧过程中形成的，而色氨酸和含有羧酸基团的β -碳碱是木材烟雾中FG 7142的前体。(3)在人尿中检测到FG 7142。我们的数据表明，人类暴露于FG 7142，吸烟者暴露于FG 7142的水平高于非吸烟者。动物实验结果表明，进入血液的fg7142在24小时内以不变的形式通过肾脏随尿液排出体外。因此，监测尿中FG 7142的水平可能有助于监测FG 7142的暴露水平。少

FG 7142 (N-methyl-beta-carboline-3-carboxamide) is an anxiogenic agent used to investigate the pathogenesis and mechanism of anxiety in man. FG 7142, classified as a partial inverse agonist at benzodiazepine receptors, produces not only a strong anxiety-like syndrome in experimental animals, but also severe anxiety in man. This project is focused on the distribution and formation mechanism of FG 7142 in the environment and also on the effect of FG 7142 in the environment on humans.We have clearly demonstrated the followings :(1) FG 7142 has been measured in cigarette smoke, airborne partcles, automobile-exhaust particles, incinerator ash, smoke condensate of tree leaves and cigarette-smoke polluted indoor air by high-performance liquid chromatography. This compound has been detected in cigarette smoke, airborne partcles, smoke condensate of tree leaves and cigarette-smoke polluted indoor air, but not in automobile-exhaust partcles, cigarette and tree leaves themselves.These findings su … More ggest that FG 7142 is widely distributed in the environment and that FG 7142 is likely to be formed through conbustion of plants.(2) FG 7142 has been detected in the smoke condensate of wood shavings which is collected by an automatic smoking mechine. However, this compound has not been detected in the methylene chloride extract of wood shavings themseleves. Moreover, the yield of FG 7142 in the smoke condensate has increased dose-dependently with the added amounts of tryptophan and beta-carbolines possessing a carboxylate moiety. These findings suggest that FG 7142 is formed during combustion of plants and that tryptophan and beta-carbolines possessing a carboxylate moiety are precursors of FG 7142 in wood smoke.(3) FG 7142 has been detected in human urine. Our data suggest that humans are exposed to FG 7142 and that smokers are exposed to higher levels of FG 7142 than non-smokers. Results of animal experiments suggest that FG 7142 which enters the blood-stream is excreted in the urine via the kidneys within 24 h in an unchanged form. Therefore, monitoring the level of FG 7142 in urine may be useful for monitoring the exposure level of FG 7142. Less