Vasar E E, Nurk A M, Maĭmets M O, Allikmets L Kh
Biull Eksp Biol Med. 1985 Jan;99(1):72-4.
It has been established in experiments on white male rats that prolonged administration (twice a day for 14 days) of haloperidol (0.25 mg/kg) and pyreneperone (0.25 mg/kg) resulted in the reduced interaction between 3H-spiroperidol and low affinity binding sites for apomorphine in subcortical structures, whereas 3H-spiroperidol binding with high affinity binding sites for apomorphine increased both in the frontal cortex and subcortical structures of the forebrain. After prolonged administration of neuroleptics the displacing effect of cerulein, an analog of cholecystokinin octapeptide, was replaced by the stimulant action on 3H-spiroperidol binding. It is assumed that increased interaction between 3H-spiroperidol and high affinity binding sites for apomorphine on dopamine2- and serotonin2-receptors underlies the antipsychotic action of neuroleptics after their prolonged administration. Cholecystokinin octapeptide is a necessary factor for realization of this action of neuroleptics.
在对白种雄性大鼠进行的实验中已证实，长期给予氟哌啶醇（0.25毫克/千克）和芘哌隆（0.25毫克/千克）（每天两次，共14天）会导致3H-螺哌啶醇与皮层下结构中阿扑吗啡低亲和力结合位点之间的相互作用减少，而3H-螺哌啶醇与阿扑吗啡高亲和力结合位点的结合在额叶皮层和前脑的皮层下结构中均增加。长期给予抗精神病药物后，八肽胆囊收缩素类似物雨蛙肽的置换作用被对3H-螺哌啶醇结合的刺激作用所取代。据推测，长期给予抗精神病药物后，3H-螺哌啶醇与多巴胺2受体和5-羟色胺2受体上阿扑吗啡高亲和力结合位点之间相互作用的增加是抗精神病药物抗精神病作用的基础。八肽胆囊收缩素是实现抗精神病药物这种作用的必要因素。
