Novel mechanism of modulation at a ligand-gated ion channel; action of 5-Cl-indole at the 5-HT₃ A receptor.

ABSTRACT:

Background and purpose

The 5-HT₃ receptor is a prototypical member of the Cys-loop ligand-gated ion channel (LGIC) superfamily and an established therapeutic target. In addition to activation via the orthosteric site, receptor function can be modulated by allosteric ligands. We have investigated the pharmacological action of Cl-indole upon the 5-HT₃ A receptor and identified that this positive allosteric modulator possesses a novel mechanism of action for LGICs.

Experimental approach

The impact of Cl-indole upon the 5-HT₃ receptor was assessed using single cell electrophysiological recordings and [³ H]-granisetron binding in HEK293 cells stably expressing the 5-HT₃ receptor.

Key results

Cl-indole failed to evoke 5

SUBMITTER: Powell AD 

PROVIDER: S-EPMC5120152 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature