Nicotinic acetylcholine receptor subunit monepantel-1 (MPTL-1)

Nicotinic acetylcholine receptor subunit monepantel‑1 (MPTL‑1), also known as ACR‑23 in Caenorhabditis elegans, is a member of the DEG‑3 subfamily of nicotinic acetylcholine receptors. These are ligand-gated ion channels found specifically in nematodes and are not present in mammals. The primary biological function is mediating signal transduction via nonselective monovalent cation conductance upon activation by agonists such as betaine or synthetic anthelmintics like monepantel. Activation leads to depolarization and subsequent paralysis of the parasite. This target is central to the mechanism of action for amino-acetonitrile derivative (AAD) class anthelmintics, with monepantel acting as a super agonist at this site[2][3]. Mutations or mis-splicing events affecting this gene confer resistance to these drugs among parasitic nematodes such as Haemonchus contortus[3]. No cross-resistance has been observed between AADs targeting this receptor and other classes like imidazothiazoles[1].

Other names

ACR-23MPTL-1Acetylcholine receptor monepantel-1

Agonist activation of the nicotinic acetylcholine receptor subunit, leading to nematode paralysis and death[2][3].