Pharmacological characterization of a homomeric nicotinic acetylcholine receptor formed by Ancylostoma caninum ACR-16
作者： Shivani Choudhary , James G. Tipton , Melanie Abongwa , Matthew T. Brewer , Jeba Jesudoss Chelladurai
DOI: 10.1007/S10158-019-0231-0
关键词: Nicotinic agonist 、 Nicotinic acetylcholine receptor 、 Receptor 、 Pharmacology 、 Cholinergic 、 Biology 、 Ancylostoma caninum 、 Homomeric 、 Acetylcholine receptor 、 Oxantel
摘要: Parasitic nematode infections are treated using anthelmintic drugs, some of which target nicotinic acetylcholine receptors (nAChRs) located in different parasite tissues. The limited arsenal agents and the prevalence drug resistance imply that future defense against parasitic will depend on discovery novel targets therapeutics. Previous studies have suggested Ascaris suum ACR-16 nAChRs a suitable for development antinematodal drugs. In this study, we characterized pharmacology Ancylostoma caninum receptor two-electrode voltage-clamp electrophysiology. This technique allowed us to study effects cholinergic agonists antagonists expressed Xenopus laevis oocytes. Aca-ACR-16 was not sensitive many existing cholinomimetic anthelmintics (levamisole, oxantel, pyrantel, tribendimidine). 3-Bromocytisine most potent agonist (> 130% control current) nAChR but, unlike Asu-ACR-16, oxantel did activate receptor. mean time constants desensitization were longer than rates observed Asu-ACR-16. contrast A. completely inhibited by DHβE moderately α-BTX. conclusion, successfully reconstituted fully functional homomeric nAChR, ACR-16, from caninum, model human hookworm infections. is distinct levamisole-sensitive receptors. homologue also displayed pharmacological differences Hence, may be valid site
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