Naber D, Wirz-Justice A, Kafka M S, Wehr T A
Psychopharmacology (Berl). 1980;68(1):1-5. doi: 10.1007/BF00426642.
To investigate diurnal variations in dopamine receptor binding, the amount of specifically bound 3H-spiroperidol was measured at 4-h intervals over a 24-h period in the striatum of rats which had been housed under a controlled 12-h light-dark cycle (lights on 7 a.m.). A highly significant ultradian rhythm with peaks at 2 a.m. and 2 p.m. was found with an amplitude of about 75%. Chronic imipramine modified the rhythm such that the two peaks occurred 4 h later and amplitude as well as 24-h mean of binding decreased. Scatchard analysis at times of least and greatest binding indicated that the differences in binding were due not to changes in the affinity, but in the number of binding sites. These results are interpreted with regard to the mode of action of psychoactive drugs and to postulated changes of receptor sensitivity in neurological and psychiatric disorders.
为研究多巴胺受体结合的昼夜变化,在处于12小时光照-黑暗周期(上午7点开灯)控制下饲养的大鼠纹状体中,每隔4小时测量一次特异性结合的3H-螺哌啶醇的量,持续24小时。发现存在一个高度显著的超日节律,在凌晨2点和下午2点出现峰值,幅度约为75%。慢性丙咪嗪改变了该节律,使得两个峰值在4小时后出现,结合的幅度以及24小时平均值均降低。在结合最少和最多时进行的Scatchard分析表明,结合的差异不是由于亲和力的变化,而是由于结合位点数量的变化。这些结果从精神活性药物的作用方式以及神经和精神疾病中假定的受体敏感性变化方面进行了解释。