Lai W S, el-Fakahany E E
Neurosci Lett. 1986 Jun 6;67(1):87-91. doi: 10.1016/0304-3940(86)90214-4.
The effect of 4-aminopyridine and its analogs on the specific binding of [3H]phencyclidine was investigated in rat brain homogenates. 4-Aminopyridine (4-AP) and 3,4-diaminopyridine displaced [3H]phencyclidine binding, while 3-aminopyridine was without effect. The concentrations of 4-AP required for inhibition of binding increased with increasing the ligand concentration, and the resultant Dixon plots indicated a competitive type of interaction. However, 4-AP also accelerated the dissociation rate of the ligand-receptor complex, suggesting that the effect of 4-AP on phencyclidine receptors in the brain might not be purely competitive.
在大鼠脑匀浆中研究了4-氨基吡啶及其类似物对[3H]苯环己哌啶特异性结合的影响。4-氨基吡啶（4-AP）和3,4-二氨基吡啶能取代[3H]苯环己哌啶的结合，而3-氨基吡啶则无此作用。抑制结合所需的4-AP浓度随配体浓度增加而升高，所得的迪克森图表明是竞争性相互作用类型。然而，4-AP也加速了配体-受体复合物的解离速率，这表明4-AP对脑中苯环己哌啶受体的作用可能并非纯粹竞争性的。
