MacKenzie R G, Zigmond M J
Eur J Pharmacol. 1985 Jul 17;113(2):159-65. doi: 10.1016/0014-2999(85)90732-0.
In vitro binding of [3H]cis(Z)-flupentixol (FPT) to rat striatal membranes was evaluated as an assay for D-1 receptors. It was found that under the appropriate assay conditions [3H]FPT bound to a single saturable site which was most abundant in striatum and bound dopaminergic agonists in the potency order that these drugs demonstrate for adenylate cyclase. These data support previous work suggesting that [3H]FPT labels the D-1 receptor. Next, rats received haloperidol or fluphenazine for 54 days and striatal dopamine receptors were assayed 72 h later. The drug treatments increased the density of D-2 receptors as measured by [3H]spiperone binding by 40% and 25% respectively. However, no change was observed in D-1 receptor density. We conclude that effects of chronic neuroleptic treatment that depend upon increased dopamine receptor density are mediated via the D-2 receptor subtype.
评估了[3H]顺式(Z)-氟哌噻吨(FPT)与大鼠纹状体膜的体外结合，作为一种检测D-1受体的方法。发现在适当的检测条件下，[3H]FPT与单个可饱和位点结合，该位点在纹状体中最为丰富，并且以这些药物对腺苷酸环化酶所显示的效力顺序结合多巴胺能激动剂。这些数据支持了先前的研究工作，表明[3H]FPT标记D-1受体。接下来，给大鼠服用氟哌啶醇或氟奋乃静54天，并在72小时后检测纹状体多巴胺受体。药物治疗使通过[3H]螺哌隆结合测定的D-2受体密度分别增加了40%和25%。然而，未观察到D-1受体密度有变化。我们得出结论，依赖于多巴胺受体密度增加的慢性抗精神病药物治疗的作用是通过D-2受体亚型介导的。
