Target intelligence / Profile preview

Nicotinic acetylcholine receptor (parasite subtype) (nAChR (parasite))

Target
nAChR (parasite)
Molecular classification
Ion channel, Receptor, Ligand-gated ion channel (Cys-loop receptor family)
01

Overview

The nicotinic acetylcholine receptor (parasite subtype) is a pentameric ligand-gated ion channel consisting of various subunit combinations unique to parasitic species. Upon binding acetylcholine or cholinergic anthelmintic drugs (such as levamisole, pyrantel, or nicotine derivatives), the receptor opens and allows the influx of cations (Na⁺, K⁺, Ca²⁺), leading to membrane depolarization and muscle contraction in the parasite. Functional diversity in the receptor arises from sequence variation and stoichiometry of the subunits, causing different pharmacological responses to drugs. Drug-resistance in parasites is often linked to mutations or altered expression of these receptor subunits. Anthelmintics targeting nAChRs remain crucial in the control of parasitic diseases in animals and humans but are threatened by rising drug resistance, emphasizing the need for novel compounds and improved characterization of parasite-specific nAChR biology[1][2][3][4][5][6].

Other names
Parasite nAChRNicotinic-sensitive acetylcholine receptor (parasite)Cholinergic receptor (parasite)N-AChR (parasite)Nicotinic receptor (parasite)
02

Mechanism of action

Agonists (e.g., levamisole, pyrantel, nicotine) bind and activate the receptor—causing sustained muscle contraction, spastic or flaccid paralysis, and death of the parasite[1][3][5][6]; Antagonists (e.g., derquantel) block receptor activation or alter receptor sensitivity[3]

03

Biological functions

Signal transductionMuscle contractionNeurotransmissionParasite movement and motility
04

Disease associations

Infection (parasitic nematode and flatworm diseases in humans and animals[1][2][3][5][6])
05

Safety considerations

Resistance due to genetic changes in nAChR subunits, leading to loss or reduction of drug efficacy[2][3][5]Potential off-target effects or toxicity in non-target organisms if host and parasite nAChRs are insufficiently distinct[2][6]
06

Interacting drugs

Levamisole

8 more in the full profile.

07

Biomarkers

Mutations or altered expression of nAChR subunits (e.g., UNC-29, UNC-38, UNC-63, ACR-8) associated with drug resistance in parasites[1][3][5]

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