Bringmann G, God R, Feineis D, Wesemann W, Riederer P, Rausch W D, Reichmann H, Sontag K H
Institute of Organic Chemistry, University of Würzburg, Federal Republic of Germany.
J Neural Transm Suppl. 1995;46:235-44.
Due to its structural analogy to the neurotoxin MPTP, "TaClo" (1-trichloromethyl-1,2,3,4-tetrahydro-beta-carboline), a compound readily originating in vitro from tryptamine ("Ta") and chloral ("Clo"), is discussed as a potential natural inducer of parkinsonian-like symptoms. Its spontaneous formation in man has to be taken into account after application of the drug chloral hydrate or after exposure to the solvent trichloroethylene. This first representative of chloral-derived heterocycles could now indeed be demonstrated to be formed in vivo after application of its putative precursors to rats. In vivo analysis of the nigrostriatal dopamine metabolism, behavioural studies, and histochemical findings as well as a strong inhibition of the complex I of the mitochondrial respiratory chain revealed the neurotoxic potential of TaClo on the dopaminergic system.
由于其与神经毒素MPTP在结构上具有相似性,“TaClo”(1-三氯甲基-1,2,3,4-四氢-β-咔啉),一种很容易在体外由色胺(“Ta”)和水合氯醛(“Clo”)生成的化合物,被认为是帕金森氏症样症状的潜在天然诱导剂。在使用水合氯醛或接触溶剂三氯乙烯后,必须考虑其在人体内的自发形成。现在确实可以证明,在将其假定的前体应用于大鼠后,这种源自水合氯醛的杂环化合物的首个代表物能够在体内形成。对黑质纹状体多巴胺代谢的体内分析、行为研究、组织化学结果以及线粒体呼吸链复合体I的强烈抑制,揭示了TaClo对多巴胺能系统的神经毒性潜力。