Effect of triazine derivatives on neuronal nicotinic receptors.

ABSTRACT: We have characterized the effect of triazine derivatives on neuronal nicotinic receptors expressed in Xenopus oocytes. All triazines investigated inhibit the current of ?7 and ?3?4 neuronal nicotinic receptors elicited by acetylcholine. The effect is concentration dependent, reversible, and noncompetitive. In contrast, some derivatives have a dual effect on ?4?2 receptors, by potentiating the currents at intermediate concentration and causing inhibition at higher concentrations. Triazine derivatives also affect the macroscopic kinetics of the heteromeric receptors ?3?4 and ?4?2 accelerating the rise and decay time course of the currents, but have no significant effect on the kinetics of homomeric ?7 receptors. Two simple kinetic models are presented. The first reproduces the effects of different concentrations of triazines both on the peak currents and on the macroscopic kinetics of ?7 with a simple inhibitory result. The second model describes the behavior of ?4?2 receptors involving a more complex dual action.

SUBMITTER: Vazquez-Romero A 

PROVIDER: S-EPMC4140594 | biostudies-literature | 2014 Aug

REPOSITORIES: biostudies-literature