Antimalarial drugs inhibit human 5-HT(3) and GABA(A) but not GABA(C) receptors.

ABSTRACT:

Background and purpose

Antimalarial compounds have been previously shown to inhibit rodent nicotinic acetylcholine (nACh) and 5-HT(3) receptors. Here, we extend these studies to include human 5-HT(3A), 5-HT(3AB), GABA(A) alpha1beta2, GABA(A) alpha1beta2gamma2 and GABA(C) rho1 receptors.

Experimental approach

We examined the effects of quinine, chloroquine and mefloquine on the electrophysiological properties of receptors expressed in Xenopus oocytes.

Key results

5-HT(3A) receptor responses were inhibited by mefloquine, quinine and chloroquine with IC(50) values of 0.66, 1.06 and 24.3 microM. At 5-HT(3AB) receptors, the potencies of mefloquine (IC(50)=2.7 microM) and quinine (15.8 microM), but not chloroquine (23.6 microM), were reduced. Mefloquine, quinine and chloroq

SUBMITTER: Thompson AJ 

PROVIDER: S-EPMC2438262 | biostudies-literature | 2008 Apr

REPOSITORIES: biostudies-literature