Fjalland B
Acta Pharmacol Toxicol (Copenh). 1978 Jan;42(1):73-6. doi: 10.1111/j.1600-0773.1978.tb02171.x.
Neuroleptics from various chemical groups and some amino acids were examined for GABA uptake-inhibiting properties in rat brain synaptosomes. The phenothiazine and thioxanthene neuroleptics inhibited GABA uptake by 50% in the concentration range of 10-30 micron. No difference in potency was found between the cis and the trans isomers of the thioxanthenes. Clozapine and particularly sulpiride were weak inhibitors of the GABA uptake process, whereas some of the butyrophenones examined exhibited rather potent effect. Secific GABA uptake inhibitors (nipecotic acid and guvacine) were as active as the most potent butyrophenones. As no significant correlation was obtained between GABA uptake-inhibiting effect of the neuroleptics and their clinical or pharmacological effects it is concluded that the influence on GABA uptake is not an important aspect of the neuroleptic action.
对来自不同化学组别的抗精神病药物和一些氨基酸进行了检测，以研究其对大鼠脑突触体中γ-氨基丁酸（GABA）摄取的抑制特性。在10 - 30微摩尔的浓度范围内，吩噻嗪类和硫杂蒽类抗精神病药物可抑制50%的GABA摄取。硫杂蒽类的顺式和反式异构体在效力上没有差异。氯氮平，尤其是舒必利，是GABA摄取过程的弱抑制剂，而所检测的一些丁酰苯类药物表现出相当强的作用。特异性GABA摄取抑制剂（尼克酸和胍基乙酸）与最有效的丁酰苯类药物活性相当。由于抗精神病药物的GABA摄取抑制作用与其临床或药理作用之间未获得显著相关性，因此得出结论，对GABA摄取的影响不是抗精神病药物作用的重要方面。
