Cys-loop receptor channel blockers also block GLIC.

ABSTRACT: The Gloeobacter ligand-gated ion channel (GLIC) is a bacterial homolog of vertebrate Cys-loop ligand-gated ion channels. Its pore-lining region in particular has a high sequence homology to these related proteins. Here we use electrophysiology to examine a range of compounds that block the channels of Cys-loop receptors to probe their pharmacological similarity with GLIC. The data reveal that a number of these compounds also block GLIC, although the pharmacological profile is distinct from these other proteins. The most potent compound was lindane, a GABA(A) receptor antagonist, with an IC₅₀ of 0.2 μM. Docking studies indicated two potential binding sites for this ligand in the pore, at the 9' or between the 0' and 2' residues. Similar experiments with picrotoxinin (IC₅₀ = 2.6 μM) and rima

SUBMITTER: Alqazzaz M 

PROVIDER: S-EPMC3244065 | biostudies-literature | 2011 Dec

REPOSITORIES: biostudies-literature