Interaction of 4-aminopyridine with [3H]phencyclidine receptors in rat brain homogenates.

W S Lai, E E el-Fakahany, Wi S. Lai, Esam E. El-Fakahany

Index: Neurosci. Lett. 67(1) , 87-91, (1986)

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Abstract

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.