Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes.
Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes.
复制标题
[3H]氟哌啶醇和[3H]多巴胺与小牛脑膜中多巴胺受体结合的特性。
作者：
D. Burt;I. Creese;S. Snyder
[ 3 H]氟哌啶醇和[ 3 H]多巴胺以可饱和方式与小牛脑的膜结合，具有高亲和力和其他特征，表明与突触后多巴胺受体相关。结合和解离速率的动力学分析产生的KD值与平衡测量。[ 3 H]多巴胺和[ 3 H]氟哌啶醇结合的区域变化是平行的，并且对应于多巴胺能神经支配的区域差异。药物特异性似乎没有不同的边缘和纹状体区之间。各种激动剂和拮抗剂对两种配体结合的相对效力与它们在多巴胺受体位点的药理学作用平行。多巴胺激动剂对[ 3 H]多巴胺的亲和力是[ 3 H]氟哌啶醇结合位点的6-38倍.相比之下，多巴胺拮抗剂对[ 3 H]氟哌啶醇的亲和力是[3 H]多巴胺结合位点的20- 12，000倍.麦角衍生物，包括d -麦角酸二乙基酰胺，和其它5-羟色胺拮抗剂对两种类型的结合都有很大的亲和力.
[ 3 H]Haloperidol and [ 3 H]dopamine bind in saturable fashion to membranes from calf brain with high affinity and other characteristics indicating an association with post-synaptic dopamine receptors. Kinetic analysis of rates of association and dissociation yields K D values in agreement with equilibrium measurements. Regional variations in [ 3 H]dopamine and [ 3 H]haloperidol binding are parallel and correspond to regional differences in dopaminergic innervation. Drug specificity does not appear to differ between limbic and striatal areas. The relative potencies of various agonists and antagonists on the binding of the two ligands parallel their pharmacological actions at dopamine receptor sites. Dopamine agonists have 6-38 times more affinity for [ 3 H]dopamine than [ 3 H]haloperidol binding sites. By contrast, dopamine antagonists have 20-12,000 times more affinity for [ 3 H]haloperidol than [ 3 H]dopamine binding sites. Ergot derivatives, including d -lysergic acid diethylamide, and other serotonin antagonists have substantial affinity for both types of binding.