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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.
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 .
Itameline (INN Tooltip International Nonproprietary Name; developmental code name RU-47213) is a non-selective muscarinic acetylcholine receptor agonist which was under development for the treatment of Alzheimer's disease and memory disorders but was never marketed. [1] [2] [3] It has been referred to as a "nootropic" (cognitive enhancer). [4] [5]
Xanomeline is an agonist that primarily targets the muscarinic acetylcholine receptor family of five muscarinic receptor subtypes, which are designated M 1-M 5. [2] While it binds with near identical affinity to all five of the muscarinic receptor subtypes as measured by displacement of a muscarinic radioligand, the preponderance of evidence suggests that xanomeline acts preferentially in the ...
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]
Preclinical data supports the hypothesis that xanomeline's central mechanism of action is mediated primarily through stimulation of brain muscarinic M 4 and M 1 receptors. [5] M 4 muscarinic receptors are most highly expressed in the midbrain, which controls motor and action planning, decision-making, motivation, reinforcement, and reward ...
Oxotremorine is a drug that acts as a selective muscarinic acetylcholine receptor agonist. [1]Oxotremorine produces ataxia, tremor and spasticity, similar to those symptoms seen in Parkinsonism, and has thus become a research tool in experimental studies aimed at determining more effective anti-Parkinsonian drugs.