Bocchetta A, Piccardi M P, Del Zompo M, Pintus S, Corsini G U
J Neurochem. 1985 Sep;45(3):673-6. doi: 10.1111/j.1471-4159.1985.tb04045.x.
A saturable, specific, high-affinity binding site for [3H]1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine was found in rat brain homogenates. The CNS regional distribution, the subcellular fractionation, and the displacement by pargyline, clorgyline, and deprenyl suggest that this binding site may correspond to monoamine oxidase. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine inhibited the oxidative deamination of dopamine, both in vivo and in vitro. Striatal levels of 3,4-dihydroxyphenylacetic acid were significantly reduced shortly after intravenous administration, and returned to normal values after a few hours. The in vitro formation of 3,4-dihydroxyphenylacetic acid from dopamine was inhibited by concentrations of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine comparable to those of pargyline.
在大鼠脑匀浆中发现了一个对[3H]1-甲基-4-苯基-1,2,3,6-四氢吡啶具有饱和性、特异性和高亲和力的结合位点。中枢神经系统区域分布、亚细胞分级分离以及帕吉林、氯吉兰和司来吉兰对其的置换作用表明，该结合位点可能与单胺氧化酶相对应。1-甲基-4-苯基-1,2,3,6-四氢吡啶在体内和体外均抑制多巴胺的氧化脱氨作用。静脉注射后不久，纹状体中3,4-二羟基苯乙酸的水平显著降低，并在数小时后恢复到正常水平。与帕吉林浓度相当的1-甲基-4-苯基-1,2,3,6-四氢吡啶浓度可抑制多巴胺体外生成3,4-二羟基苯乙酸。
