Bhargava H N, Perlow M J
Department of Pharmacodynamics, University of Illinois at Chicago 60612.
Toxicol Lett. 1988 Mar;40(3):219-24. doi: 10.1016/0378-4274(88)90044-6.
The effect of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), a neurotoxin which selectively destroys the nigrostriatal dopaminergic neurons and produces Parkinson's disease-like syndrome, on striatal dopamine receptors was determined in a mouse strain known to be very sensitive to the neurotoxic effect of MPTP. Daily intraperitoneal administration of MPTP (30 mg/kg) for 7 days to male C57BL/6 mice reduced the concentration of striatal dopamine by 90%. This decrease in dopamine concentration was not associated with changes either in the receptor density (Bmax) or the apparent dissociation constant (Kd) of [3H]spiroperidol to bind to striatal dopamine receptors. It is concluded that in spite of large decrease in striatal dopamine concentration by MPTP the dopamine receptors labeled with [3H]spiroperidol remain intact.
1-甲基-4-苯基-1,2,3,6-四氢吡啶（MPTP）是一种神经毒素，可选择性破坏黑质纹状体多巴胺能神经元并产生帕金森病样综合征。在已知对MPTP神经毒性作用非常敏感的小鼠品系中，测定了MPTP对纹状体多巴胺受体的影响。对雄性C57BL/6小鼠每日腹腔注射MPTP（30mg/kg），持续7天，可使纹状体多巴胺浓度降低90%。多巴胺浓度的这种降低与[3H]螺哌啶醇与纹状体多巴胺受体结合的受体密度（Bmax）或表观解离常数（Kd）的变化均无关。得出的结论是，尽管MPTP使纹状体多巴胺浓度大幅降低，但用[3H]螺哌啶醇标记的多巴胺受体仍保持完整。
