Abstract
Ligand-gated ion channels (LGIC) allow rapid responses in the nervous system. The nicotonic acetylcholine receptor (AChR) has been the model for structure-function relationship studies on this superfamily. The AChR undergoes the following functional events:
-
1.
Binding of the neurotransmitter.
-
2.
Opening of the ion channel.
-
3.
Conduction of ions across the pore.
-
4.
Desensitization.
The equilibrium among these processes can be perturbed by alteration in the primary structure of the AChR or by the presence of pharmacological agents.
Changes in the primary sequence leading to modifications in gating kinetics may occur in association with physiological or pathological processes. Such changes can also be genetically engineered to gain insights into structure-function relationships.
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Abbreviations
- AChR:
-
nicotinic cholinergic receptor
- LGIC:
-
ligand-gated ion channels
- NCI:
-
noncompetitive inhibitor
- PCP:
-
phencyclidine
- HEK:
-
cells, human embryonic kidney cells
- CMS:
-
congenital myasthenic syndrome
- SCCMS:
-
slow-channel congenital myasthenic syndrome
- TID:
-
3-(trifluoromethyl)3-m-(iodophenyl)diazirine
- HC:
-
hydrocortisone
- BSA:
-
bovine serum albumin
- τon :
-
mean open time
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Bouzat, C., Barrantes, F.J. Inherited and experimentally induced changes in gating kinetics of muscle nicotinic acetylcholine receptor. J Mol Neurosci 13, 1–16 (1999). https://doi.org/10.1385/JMN:13:1-2:1
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DOI: https://doi.org/10.1385/JMN:13:1-2:1