Boswell R F, Welstead W J, Duncan R L, Johnson D N, Funderburk W H
J Med Chem. 1978 Jan;21(1):136-9. doi: 10.1021/jm00199a029.
In previous studies the phenyl-4-piperidinylmethanone moiety was shown to be a neuroleptic pharmacophore. A short series of [1-[3-(phenothiazin-10-yl)propyl]-4-piperidinyl]phenylmethanones was prepared and tested for neuroleptic activity using the blockade of d-amphetamine lethality in aggregated mice and suppression of conditioned avoidance behavior as the end points. Most compounds were shown to be potent neuroleptic agents and two were found to possess a long duration of action.
在先前的研究中，苯基 - 4 - 哌啶基甲酮部分被证明是一种抗精神病药效基团。制备了一系列短链的[1 - [3 - (吩噻嗪 - 10 - 基)丙基] - 4 - 哌啶基]苯基甲酮，并以聚集小鼠中d - 苯丙胺致死性的阻断和条件性回避行为的抑制作为终点来测试其抗精神病活性。大多数化合物被证明是有效的抗精神病药物，并且发现有两种具有长效作用。
