Target intelligence / Profile preview

Oxantel-sensitive nicotinic acetylcholine receptor (O-AChR)

Target
O-AChR
Molecular classification
Ion channel, Ligand-gated ion channel, Nicotinic acetylcholine receptor, Cys-loop ligand-gated ion channel
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Overview

The oxantel-sensitive nicotinic acetylcholine receptor (O-AChR) is a specialized ligand-gated ion channel primarily identified in Clade I parasitic nematodes, such as the whipworm species Trichuris suis and Trichuris trichiura [1, 2]. It is a pentameric protein, typically forming a homomeric assembly of ACR-16-like subunits, which distinguishes it from the nicotinic receptors found in other nematode clades [2, 5]. Biologically, the receptor mediates fast excitatory neurotransmission at the neuromuscular junction, where its activation triggers cation influx and subsequent muscle contraction [1, 4]. In the context of human and veterinary medicine, this receptor is the primary therapeutic target for the anthelmintic drug oxantel, which is used to treat trichuriasis (whipworm infection) [1, 3]. Oxantel acts as a potent and selective agonist of the O-AChR, inducing persistent membrane depolarization that leads to spastic paralysis and the eventual expulsion of the parasite from the host's gastrointestinal tract [1, 2]. While related to the nicotine-sensitive (N-type) and levamisole-sensitive (L-type) receptors, the O-AChR's unique pharmacological profile explains the high efficacy of oxantel against whipworms compared to other broad-spectrum anthelmintics [2, 5].

Other names
O-type nicotinic acetylcholine receptorO-subtype nAChRACR-16-like nicotinic acetylcholine receptorOxantel-sensitive nAChRO-AChR
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Mechanism of action

Selective agonist that induces persistent depolarization and spastic paralysis

03

Biological functions

Neuromuscular signalingMuscle contractionExcitatory neurotransmissionLocomotion
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Disease associations

InfectionTrichuriasisSoil-transmitted helminthiasis
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Safety considerations

Narrow spectrum of activity (primarily effective against Trichuris)Potential for anthelmintic resistancePotential cross-reactivity with host nicotinic receptors at high concentrations
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Interacting drugs

Oxantel

5 more in the full profile.

07

Biomarkers

Egg reduction rate (ERR)Cure rate (CR)

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