Abstract: AIM: To investigate the reactivation of neuronal α4β2-nicotinic acetylcholine receptors following desensitization induced by agonist and the antagonism of benthiactzine against it .METHODS: The whole cell recording configuration of patch-clamp technique and the rapid application of nicotine were performed in α4β2-nAChRs heterologously expressed in cultured SH-EP1 cells. RESULTS: An inward current was elicited by rapid application of 1 mmol/L nicotine in SH-EP1 cells.This current reached peak rapidly and then desensitized fast when the application of agonist was prolonged. However, after the removal of nic-otine, an additional inward current reoccurred. This rebound current can be blocked by benthiactzine, a new antagonist of cholinergic receptors. CONCLUSION: Neuronal α4β2-nicotinic acetylcholine receptor heterologously expressed in the SH-EP1 cell line can be desensitized by prolonged agonist application, and be reactivated after the removal of agonist .This reactivat-ed current can be blocked by benthiactzine, a new an- tagonist of cholinergic receptors.

Key words: nicotinic acetylcholine receptors, or-ganophosphate poisoning, rebound, benthiactzine, patch clamp