Zharkovskiĭ A M, Zharkovskaia T A
Biull Eksp Biol Med. 1984 Oct;98(10):457-9.
It has been demonstrated in experiments on rats receiving chronic (16 days) treatment with haloperidol (1.0 mg/kg/day), sulpiride (50 mg/kg/day) and clozapine (10 mg/kg/day) that binding of 3H-flunitrazepam in the striatum, limbic system, and cortex is reduced at the 5th day after withdrawal of the neuroleptics. That release was determined by the diminution of the number of receptors without changing in the dissociation constant. The reduction in the density of benzodiazepine receptors (BD-receptors) after withdrawal of the neuroleptics attests to their agonistic effect on BD-receptors. Apparently these changes are not linked with a direct effect of the neuroleptics on BD-receptors, since they displace 3H-flunitrazepam in experiments in vitro only at micromolar concentrations. It is assumed that the reduction in 3H-flunitrazepam binding is mediated via the GABAergic system transsynaptically in response to increase in the number of dopamine (neuroleptic) receptors.
在对接受氟哌啶醇（1.0毫克/千克/天）、舒必利（50毫克/千克/天）和氯氮平（10毫克/千克/天）慢性（16天）治疗的大鼠进行的实验中表明，在停用抗精神病药物后的第5天，纹状体、边缘系统和皮质中3H-氟硝西泮的结合减少。这种释放是由受体数量减少决定的，而解离常数没有变化。停用抗精神病药物后苯二氮䓬受体（BD受体）密度的降低证明了它们对BD受体的激动作用。显然，这些变化与抗精神病药物对BD受体的直接作用无关，因为它们仅在微摩尔浓度下才会在体外实验中取代3H-氟硝西泮。据推测，3H-氟硝西泮结合的减少是通过GABA能系统经突触介导的，以响应多巴胺（抗精神病药物）受体数量的增加。
