Balakleevskiĭ A I, Maslova I V
Biull Eksp Biol Med. 1978 Apr;85(4):429-31.
Neuroleptics (haloperidol) closapine, pimozid, chlorpromazine) diminished the level of free (functionally active) form of acetylcholine (ACh), and, to some extent, the bound form of ACh; they changed the content of the labile-bound (vesicular) form of ACh and weakly influenced the choline-acetyltranspherase activity in the basal ganglia of the rat brain 5 to 30 min after the injection. In contrast to the inhibitory action on the acetyl-cholinesterase (AChE) activity in vitro, most of the neuroleptics, except closapine, increased the AChE activity in vivo. These results indicate that the neuroleptics activate ACh-metabolism and probably stimulate the cholinergic structure in the basal ganglia of the brain; the AChE activity may serve as a criterion of such stimulating action of neuroleptics.
抗精神病药物(氟哌啶醇、氯氮平、匹莫齐特、氯丙嗪)降低了乙酰胆碱(ACh)游离(功能活性)形式的水平,并在一定程度上降低了ACh结合形式的水平;它们改变了ACh不稳定结合(囊泡)形式的含量,并在注射后5至30分钟对大鼠脑基底神经节中的胆碱乙酰转移酶活性产生微弱影响。与体外对乙酰胆碱酯酶(AChE)活性的抑制作用相反,除氯氮平外,大多数抗精神病药物在体内增加了AChE活性。这些结果表明,抗精神病药物激活了ACh代谢,可能刺激了脑基底神经节中的胆碱能结构;AChE活性可能作为抗精神病药物这种刺激作用的一个标准。