Nagai Y, Irie A, Masuda Y, Oka M, Uno H
J Med Chem. 1979 Jun;22(6):677-83. doi: 10.1021/jm00192a013.
The synthesis and some pharmacological effects of cis- and trans-2-substituted 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivatives are described. In these derivatives, the substituents of the 2, 5 and 8 position, together with the relative configuration of the 4a and 9b position, influenced the potency of the central nervous system activities. A cis-2-[3-(p-fluorobenzoyl)propyl] analogue (5k) of carbidine (1) possessed not only thymoleptic-like biological activity but had more potent neuroleptic activity than the parent drug.
描述了顺式和反式-2-取代的2,3,4,4a,5,9b-六氢-1H-吡啶并[4,3-b]吲哚衍生物的合成及其一些药理作用。在这些衍生物中，2、5和8位的取代基以及4a和9b位的相对构型影响中枢神经系统活性的效力。卡比定（1）的顺式-2-[3-（对氟苯甲酰基）丙基]类似物（5k）不仅具有类抗抑郁生物活性，而且比母体药物具有更强的抗精神病活性。
