Acetylcholine receptor
From Pharmpedia
An acetylcholine receptor (abbreviated AChR) is an integral membrane protein that responds to the binding of the neurotransmitter acetylcholine.
Classification
Like other transmembrane receptors, acetylcholine receptors are classified according to their "pharmacology", or according to their relative affinities and sensitivities to different molecules. Although all acetylcholine receptors, by definition, respond to acetylcholine, they respond to other molecules as well.
- nicotinic acetylcholine receptors (nAChR, also known as "ionotropic" acetylcholine receptors) are particularly responsive to nicotine
- muscarinic acetylcholine receptors (mAChR, also known as metabotropic acetylcholine receptors) are particularly responsive to muscarine.
Receptor types
Molecular biology has shown that the nicotinic and muscarinic receptors belong to distinct protein superfamilies.
The nAChRs are ion channels, and like other members of the "cys-loop" ligand-gated ion channel superfamily, are composed of five protein subunits arranged like staves around a barrel. The subunit composition is highly variable across different tissues.
In contrast, the mAChRs are not ion channels, but belong instead to the superfamily of G-protein coupled receptors that activate other ionic channels via a second messenger cascade.
Role in health and disease
Nicotinic acetylcholine receptors can be blocked by curare and toxins present in the venoms of snakes and shellfishes. Drugs such as the neuromuscular blocking agents bind reversibly to the nicotinic receptors in the neuromuscular junction and are used routinely in anaesthesia.
Nicotinic receptors are the main mediator of nicotine and tobacco addiction. In myasthenia gravis, the receptor is targeted by antibodies, leading to muscle weakness. Muscarinic acetylcholine receptors can be blocked by the drugs atropine and scopolamine.
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