Torreilles J, Guérin M C, Previero A
Biochimie. 1985 Sep;67(9):929-47. doi: 10.1016/s0300-9084(85)80289-3.
We reviewed the origins, the synthetic pathways and the biological properties of beta-carbolines, the condensation products of tryptophan and indole alkylamines with aldehydes. They were found in many plants, some of which have been used as hallucinogens. They also occur as minor constituents in tobacco smoke. In mammalian body, beta-carboline derivatives occur normally in plasma, platelets and urine, moreover it seems that some are formed in human body after alcohol intake. Due to interesting biological effects described in recent years (inhibition of monoamine oxidase, binding to benzodiazepine receptors, comutagenic and carcinogenic properties, 5-hydroxy tryptamine uptake inhibition), many attempts were made to prepare beta-carbolines starting from various indole derivatives. We reviewed the published methods up to 1975 and summarized the main patents related with pharmacological properties of synthetic beta-carbolines.
我们回顾了β-咔啉的起源、合成途径及其生物学特性，β-咔啉是色氨酸和吲哚烷基胺与醛的缩合产物。它们存在于许多植物中，其中一些被用作致幻剂。它们也是烟草烟雾中的微量成分。在哺乳动物体内，β-咔啉衍生物通常存在于血浆、血小板和尿液中，此外，似乎有些是在人体摄入酒精后形成的。由于近年来所描述的有趣生物学效应（抑制单胺氧化酶、与苯二氮䓬受体结合、共诱变和致癌特性、抑制5-羟色胺摄取），人们进行了许多尝试，从各种吲哚衍生物开始制备β-咔啉。我们回顾了截至1975年已发表的方法，并总结了与合成β-咔啉药理特性相关的主要专利。
