Article
The influence of allosteric modulators and transmembrane mutations on desensitisation and activation of α7 nicotinic acetylcholine receptors.
Neuropharmacology - 1 Oct 2015
Chatzidaki Anna, D'Oyley Jarryl M, Gill-Thind JasKiran K, Sheppard Tom D, Millar Neil S
Abstract excerpt
Acetylcholine activates nicotinic acetylcholine receptors (nAChRs) by binding at an extracellular orthosteric site. Previous studies have described several positive allosteric modulators (PAMs) that are selective for homomeric α7 nAChRs. These include type I PAMs, which exert little or no effect on the rate of receptor desensitisation, and type II PAMs, which cause a dramatic loss of agonist-induced...
Topics
- Acetylcholine
- Allosteric Site
- Animals
- Cholinergic Agents
- HEK293 Cells
- Humans
- Membrane Potentials
- Mice
- Molecular Structure
- Mutation
- Oocytes
- Radioligand Assay
- Rats
- Receptors, Serotonin, 5-HT3
- Xenopus laevis