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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Acetylcholine is familiar as a neurotransmitter in the central nervous system and in the periphery. In the somatic nervous system, it activates nicotinic acetylcholine receptors at the skeletal neuromuscular junction. It is also employed in the autonomic nervous system, in both parasympathetic and sympathetic branches; in the former, at the smooth muscle neuromuscular junction, activating muscarinic acetylcholine receptors. In the latter, acetylcholine is involved as a neurotransmitter at the ganglion, activating nicotinic acetylcholine receptors. Acetylcholine is synthesised in neurones through the action of choline O-acetyltransferase and metabolised after release through the extracellular action of acetylcholinesterase and cholinesterase. Choline is accumulated from the extracellular medium by selective transporters (see SLC5A7 and the SLC44 family). Acetylcholine is accumulated in synaptic vesicles through the action of the vesicular acetylcholine transporter SLC18A3.
* Key recommended reading is highlighted with an asterisk
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Deiana S, Platt B, Riedel G. (2011) The cholinergic system and spatial learning. Behav. Brain Res., 221 (2): 389-411. [PMID:21108971]
* Engel AG, Shen XM, Selcen D, Sine SM. (2015) Congenital myasthenic syndromes: pathogenesis, diagnosis, and treatment. Lancet Neurol, 14 (4): 420-34. [PMID:25792100]
Giacobini E. (2003) Cholinesterases: new roles in brain function and in Alzheimer's disease. Neurochem. Res., 28 (3-4): 515-22. [PMID:12675140]
Kawashima K, Fujii T, Moriwaki Y, Misawa H. (2012) Critical roles of acetylcholine and the muscarinic and nicotinic acetylcholine receptors in the regulation of immune function. Life Sci., 91 (21-22): 1027-32. [PMID:22659391]
León R, Garcia AG, Marco-Contelles J. (2013) Recent advances in the multitarget-directed ligands approach for the treatment of Alzheimer's disease. Med Res Rev, 33 (1): 139-89. [PMID:21793014]
* Rosini M, Simoni E, Minarini A, Melchiorre C. (2014) Multi-target design strategies in the context of Alzheimer's disease: acetylcholinesterase inhibition and NMDA receptor antagonism as the driving forces. Neurochem. Res., 39 (10): 1914-23. [PMID:24493627]
Schliebs R, Arendt T. (2011) The cholinergic system in aging and neuronal degeneration. Behav. Brain Res., 221 (2): 555-63. [PMID:21145918]
* Zimmermann M. (2013) Neuronal AChE splice variants and their non-hydrolytic functions: redefining a target of AChE inhibitors?. Br. J. Pharmacol., 170 (5): 953-67. [PMID:23991627]
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Database page citation:
Acetylcholine turnover. Accessed on 30/03/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=765.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol. 172: 6024-6109.