Wang S S, Ricaurte G A, Peroutka S J
Eur J Pharmacol. 1987 Jun 26;138(3):439-43. doi: 10.1016/0014-2999(87)90485-7.
The binding of [3H]3,4-methylenedioxymethamphetamine [( 3H]MDMA) to both rat brain membrane preparations and glass fiber filter papers was analyzed in the present study. Saturation studies indicate that [3H]MDMA binding is saturable and monophasic in both the presence and absence of rat brain membranes. This apparent 'specific' binding of [3H]MDMA in both the presence and absence of brain homogenates was totally eliminated by pretreating glass fiber filter papers with polyethylenimine. Drug competition studies demonstrated that [3H]MDMA binding displays a distinct 'pharmacological' profile in the absence of brain tissue. These data indicate that apparent [3H]MDMA binding to rat brain homogenates results from artifactual of [3H]MDMA to glass fiber filter paper. In addition, uptake of [3H]MDMA into rat brain synaptosomes could not be detected. We conclude the [3H]MDMA has limited usefulness in radioligand binding studies.
本研究分析了[3H]3,4-亚甲基二氧甲基苯丙胺([3H]MDMA)与大鼠脑膜制剂及玻璃纤维滤纸的结合情况。饱和研究表明,无论有无大鼠脑膜,[3H]MDMA结合均具有饱和性且呈单相性。在有无脑匀浆的情况下,[3H]MDMA这种明显的“特异性”结合,通过用聚乙烯亚胺预处理玻璃纤维滤纸可完全消除。药物竞争研究表明,在无脑组织时,[3H]MDMA结合呈现出独特的“药理学”特征。这些数据表明,[3H]MDMA与大鼠脑匀浆的明显结合是[3H]MDMA与玻璃纤维滤纸之间人为作用的结果。此外,未检测到[3H]MDMA被大鼠脑突触体摄取。我们得出结论,[3H]MDMA在放射性配体结合研究中的用途有限。