Effects of glutamate and ivermectin on single glutamate-gated chloride channels of the parasitic nematode H. contortus.

ABSTRACT: Ivermectin (IVM) is a widely-used anthelmintic that works by binding to and activating glutamate-gated chloride channel receptors (GluClRs) in nematodes. The resulting chloride flux inhibits the pharyngeal muscle cells and motor neurons of nematodes, causing death by paralysis or starvation. IVM resistance is an emerging problem in many pest species, necessitating the development of novel drugs. However, drug optimisation requires a quantitative understanding of GluClR activation and modulation mechanisms. Here we investigated the biophysical properties of homomeric α (avr-14b) GluClRs from the parasitic nematode, H. contortus, in the presence of glutamate and IVM. The receptor proved to be highly responsive to low nanomolar concentrations of both compounds. Analysis of single receptor act

SUBMITTER: Atif M 

PROVIDER: S-EPMC5638611 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature