Rao M L, Deister A, Roth A
Universitätsnervenklinik, Psychiatrie, Bonn, FRG.
Pharmacopsychiatry. 1990 Jul;23(4):176-81. doi: 10.1055/s-2007-1014503.
We investigated 3H- and 125I-spiroperidol binding to lymphocytes from healthy subjects and schizophrenic patients and compared it with that to a porcine striatum dopaminergic D2-receptor preparation using identical conditions. Incubation for 60 min at 37 degrees C reduced lymphocyte 3H-spiroperidol binding to 29% of its maximal value. Binding of 3H- and 125I-spiroperidol to striatal membranes was saturable and showed high affinity; the apparent half-maximal saturation constants, KD, were 0.5 nmol/l and 1.0 nmol/l respectively for the two ligands. Lymphocyte membranes did not possess high-affinity binding sites for 3H-spiroperidol; binding to intact lymphocytes was saturable in the micromolar range; the KD values of healthy subjects and schizophrenic patients were similar. Validating all lymphocyte binding studies by parallel experiments with a striatal receptor preparation showed that human lymphocytes do not possess physiologically relevant high-affinity spiroperidol receptors.
我们研究了³H-和¹²⁵I-螺哌啶醇与健康受试者及精神分裂症患者淋巴细胞的结合情况，并在相同条件下将其与猪纹状体多巴胺能D2受体制剂的结合情况进行比较。在37℃孵育60分钟可使淋巴细胞³H-螺哌啶醇结合降至其最大值的29%。³H-和¹²⁵I-螺哌啶醇与纹状体膜的结合是可饱和的，且显示出高亲和力；两种配体的表观半数最大饱和常数KD分别为0.5 nmol/L和1.0 nmol/L。淋巴细胞膜不具有³H-螺哌啶醇的高亲和力结合位点；与完整淋巴细胞的结合在微摩尔范围内是可饱和的；健康受试者和精神分裂症患者的KD值相似。通过与纹状体受体制剂进行平行实验来验证所有淋巴细胞结合研究，结果表明人类淋巴细胞不具有生理相关的高亲和力螺哌啶醇受体。
