抗胆碱酯酶活性的比较研究几种抗精神病药物。
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Nasello AG)、基大利D, pontes低频
抗胆碱酯酶活性的比较研究几种抗精神病药物。
物化学Behav杂志》2003年7月,75 (4):895 - 901。
- PubMed ID
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12957233 (在PubMed]
- 文摘
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药物抑制血浆和组织胆碱酯酶活性是评价大鼠。多巴胺受体拮抗剂氟哌啶醇(光环),氯丙嗪(CPZ)、甲硫哒嗪(黄),氟奋乃静(流感),氯氮平(CLO)和舒必利(SULP),用作神经松驰剂,进行了测试。两个测量体外生化参数:最小有效浓度(MEC)对胆碱酯酶抑制和50%抑制浓度(IC50)。此外,动物被检测旋转活动后单方面intrastriatal注射的药物。每个药物的剂量使用以前IC50s决定。单方面纹状体药物注射后,老鼠的挑战与腹腔内注射安非他命为了刺激旋转。所有药物测试诱导减少胆碱酯酶活性。含硫的等离子体MEC,流感,光环和CPZ明显低于CLO和SULP。在纹状体,TIO的MEC CPZ和流感明显低于哈尔。根据等离子体IC50,含硫的CPZ和CLO是强有力的胆碱酯酶抑制剂。 CLO showed the lowest potency of cholinesterase inhibition in the striatum and THIO showed the highest potency in plasma and striatum. In conclusion, anticholinesterase activity is not related to D(2) receptor blockade or antipsychotic potency; and therefore the antipsychotic effects are not related to an increase in acetylcholine. All drugs induced similar contralateral rotation, except for CLO that was different from SULP and was not different from its control. Since equivalent cholinesterase inhibitory concentrations were used for all drugs and no differences in nigrostriatal behavioral effects were observed, these data suggest the participation of an important cholinergic component in this behavior. Therapeutically, the stronger the cholinesterase inhibition is, the more potent the cholinergic effects are and, consequently, the induction of extrapyramidal symptoms becomes more feasible.