Abstract
Cartap, the synthetic analog of nereistoxin, is known to act on the nicotinic acetylcholine receptor-channel (AChR). Effects of cartap on the neuronal nicotinic AChR of clonal rat phaeochromocytoma (PC 12) cells were studied using a single-channel patch clamp method. When cartap was co-applied with acetylcholine, the single-channel openings were shortened and occurred in bursts separated by brief closures or gaps. The current amplitudes in the presence of cartap were virtually identical to those of currents induced by ACh only. Mean open time and burst duration were significantly decreased in the presence of cartap in a dose-dependent manner. These changes of single-channel kinetics result in a significant decrease in total charge carried through the open AChR explaining the suppressive effect of cartap on nicotinic AChR. Results suggest that cartap could act as an open channel blocker at the nicotinic AChR.
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