Mao C C, Marco E, Revuelta A, Bertilsson L, Costa E
Biol Psychiatry. 1977 Jun;12(3):359-71.
The turnover rate of GABA is measured in substantia nigra, globus pallidus, N. accumbens, and striatum of rats injected with muscimol, a potent GABA agonist, and diazepam. The similarity of action of the two drugs on GABA turnover further supports the theory that diazepam acts as a GABA-mimetic drug. Haloperidol and clozapine affect GABA turnover differently in different nuclei. Haloperidol decreases GABA turnover in caudate but does not affect that in substantia nigra, whereas clozapine increases GABA turnover in both areas. However, both drugs accelerate GABA turnover in globus pallidus and N. accumbens. It is suggested that an increase of GABA turnover and perhaps of GABA release in striatum and substantia nigra may account for the lack of tardive dyskinesia and extrapyramidal side effects of clozapine.
在注射了强效GABA激动剂蝇蕈醇和地西泮的大鼠的黑质、苍白球、伏隔核和纹状体中测量GABA的周转率。这两种药物对GABA周转率的作用相似,进一步支持了地西泮作为一种GABA模拟药物的理论。氟哌啶醇和氯氮平在不同核团中对GABA周转率的影响不同。氟哌啶醇降低尾状核中的GABA周转率,但不影响黑质中的GABA周转率,而氯氮平则增加这两个区域的GABA周转率。然而,两种药物都能加速苍白球和伏隔核中的GABA周转率。有人提出,纹状体和黑质中GABA周转率的增加以及可能的GABA释放增加,可能是氯氮平缺乏迟发性运动障碍和锥体外系副作用的原因。