The antimalarial drugs quinine, chloroquine and mefloquine are antagonists at 5-HT3 receptors.

ABSTRACT:

Background and purpose

The antimalarial compounds quinine, chloroquine and mefloquine affect the electrophysiological properties of Cys-loop receptors and have structural similarities to 5-HT(3) receptor antagonists. They may therefore act at 5-HT(3) receptors.

Experimental approach

The effects of quinine, chloroquine and mefloquine on electrophysiological and ligand binding properties of 5-HT(3A) receptors expressed in HEK 293 cells and Xenopus oocytes were examined. The compounds were also docked into models of the binding site.

Key results

5-HT(3) responses were blocked with IC (50) values of 13.4 microM, 11.8 microM and 9.36 microM for quinine, chloroquine and mefloquine. Schild plots indicated quinine and chloroquine behaved competitively with pA (2) values of 4.

SUBMITTER: Thompson AJ 

PROVIDER: S-EPMC1994240 | biostudies-literature | 2007 Jul

REPOSITORIES: biostudies-literature