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Acetylcholine Receptor, Nematode Type L (L-AChR)

Target
L-AChR
Molecular classification
Ligand-gated ion channel, Receptor
01

Overview

The nematode L-type acetylcholine receptor (L-AChR) is a ligand-gated ion channel found at the neuromuscular junctions of nematodes. It mediates excitatory neurotransmission and is a primary target for several anthelmintic drugs, notably levamisole and pyrantel. The L-AChR is pharmacologically distinct from other nicotinic acetylcholine receptor (nAChR) subtypes in nematodes. The functional L-AChR is a pentamer composed of five different subunits: three α-subunits (unc-38, unc-63, lev-8) and two non-α-subunits (unc-29, lev-1). Assembly and trafficking of this receptor require three ancillary proteins: RIC-3, UNC-50, and UNC-74. Activation leads to depolarization of muscle cells resulting in contraction. Resistance to these drugs often maps genetically to mutations or deletions in one or more of the five core subunit genes or ancillary protein genes required for proper assembly/functioning of the receptor complex.

Other names
Levamisole-sensitive nAChRNematode L-type acetylcholine receptor
02

Mechanism of action

Agonist-induced ion channel opening leading to muscle cell depolarization and contraction (Levamisole, Pyrantel). Allosteric Inhibition (Nicotine)

03

Biological functions

Excitatory neurotransmissionMuscle contractionNeuromuscular junction signaling
04

Disease associations

Infection (Nematode)Drug Resistance (Anthelmintic)
05

Safety considerations

Drug resistance development via mutations in subunit genes or ancillary protein genes.Potential for off-target effects if similar receptors exist in non-target organisms.
06

Interacting drugs

Levamisole

2 more in the full profile.

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