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Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons [1] and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibers .
The muscarinic acetylcholine receptor M 2, also known as the cholinergic receptor, muscarinic 2, is a muscarinic acetylcholine receptor that in humans is encoded by the CHRM2 gene. [5] Multiple alternatively spliced transcript variants have been described for this gene. [5] It is G i-coupled, reducing intracellular levels of cAMP.
The muscarinic acetylcholine receptor M 1, also known as the cholinergic receptor, muscarinic 1, is a muscarinic receptor that in humans is encoded by the CHRM1 gene. [5] It is localized to 11q13. [5] This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve, [6] is common in exocrine glands and in the CNS. [7] [8]
The M 4 muscarinic receptor has been found to be a regulator of erythroid progenitor cell differentiation. Inhibition of the M 4 muscarinic receptor provides therapeutic benefits in myelodysplastic syndrome and anemia. [14] [15] [16]
The muscarinic M 3 receptor regulates insulin secretion from the pancreas [7] and are an important target for understanding the mechanisms of type 2 diabetes mellitus.. Some antipsychotic drugs that are prescribed to treat schizophrenia and bipolar disorder (such as olanzapine and clozapine) have a high risk of diabetes side-effects.
Neuronal-type receptors are located in autonomic ganglia (both sympathetic and parasympathetic), and in the central nervous system. Muscarinic acetylcholine receptors have a more complex mechanism, and affect target cells over a longer time frame. In mammals, five subtypes of muscarinic receptors have been identified, labeled M1 through M5.
The human muscarinic acetylcholine receptor M 5, encoded by the CHRM5 gene, is a member of the G protein-coupled receptor superfamily of integral membrane proteins. It is coupled to G q protein. [ 5 ]
A muscarinic acetylcholine receptor agonist, also simply known as a muscarinic agonist or as a muscarinic agent, is an agent that activates the activity of the muscarinic acetylcholine receptor. [1] The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation.