Target intelligence / Profile preview

Levamisole-sensitive nicotinic acetylcholine receptor (L-AChR)

Target
L-AChR
Molecular classification
Ion channel, Ligand-gated ion channel, Nicotinic acetylcholine receptor family
01

Overview

The Levamisole-sensitive nicotinic acetylcholine receptor (L-AChR) is a pentameric ligand-gated ion channel primarily located on the body-wall muscles of nematodes [1, 7]. It serves as the primary therapeutic target for the anthelmintic drug levamisole, which acts as a potent agonist, inducing persistent channel opening, cation influx, and spastic paralysis of the parasite [8, 16]. In the model organism Caenorhabditis elegans, the receptor is composed of five subunits (UNC-38, UNC-63, UNC-29, LEV-1, and LEV-8), although the specific subunit arrangement and composition in various parasitic species can vary and remain a subject of ongoing research [10, 12]. Beyond its role in parasites, levamisole is known to inhibit human tissue-nonspecific alkaline phosphatase (TNAP) and exert immunomodulatory effects on T-cells and macrophages, which led to its historical use in cancer and autoimmune therapy [2, 5, 8]. However, its clinical use in humans has been largely discontinued due to serious safety concerns, most notably agranulocytosis and vasculitis [8, 16]. The receptor's plasticity and the emergence of resistance in livestock parasites continue to drive research into its molecular structure and the development of new cholinergic anthelmintics [1, 12].

Other names
Levamisole receptorL-type nicotinic acetylcholine receptorNematode nicotinic acetylcholine receptorNematode nAChRUNC-38/UNC-63/UNC-29/LEV-1/LEV-8 complex
02

Mechanism of action

Agonist; induces persistent opening of the ion channel, leading to spastic paralysis in nematodes.

03

Biological functions

Neuromuscular transmissionMuscle contractionIon transportSignal transduction
04

Disease associations

InfectionHelminthiasisAscariasisHookworm infection
05

Safety considerations

Drug resistance in nematodesAgranulocytosisLevamisole-induced vasculitisNeurological side effects
06

Interacting drugs

Levamisole

5 more in the full profile.

07

Biomarkers

Parasite egg count (FECR)Worm burdenAlkaline phosphatase activityT-cell count

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