Encyclopedia of Signaling Molecules

2018 Edition
| Editors: Sangdun Choi

Acetylcholine (Nicotinic) Receptor

  • Josephine R. Tarren
  • Joan Y. Holgate
  • Selena E. BartlettEmail author
Reference work entry
DOI: https://doi.org/10.1007/978-3-319-67199-4_101538


Historical Background

The pharmacological effects of nicotine have long been known, with nicotine first isolated from tobacco plants by Posselt and Reimann in 1828 (Albuquerque et al. 2009). The attempts to isolate the physiologic effect of nicotinic acetylcholine receptors (nAChRs) using the Torpedoorganism have been traced back as far as 1885 (Paul Ehrlich) and 1857 (Claude Bernard). It was first proposed to be a protein in 1955 by David Nachmansohn and later biochemically characterized by Changeux, Kasai, and Lee in 1970. In 1983 it became the first ligand-gated ion channel for which the DNA and protein were further defined by using molecular genetics. (For more information on the history of the discovery of nAChRs...

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  1. Albuquerque EX, Pereira EF, Alkondon M, Rogers SW. Mammalian nicotinic acetylcholine receptors: from structure to function. Physiol Rev. 2009;89:73–120.  https://doi.org/10.1152/physrev.00015.2008.CrossRefPubMedPubMedCentralGoogle Scholar
  2. Alves LA, da Silva JHM, Ferreira DNM, Fidalgo-Neto AA, Teixeira PCN, de Souza CAM, et al. Structural and molecular modeling features of P2X receptors. Int J Mol Sci. 2014;15:4531–49.  https://doi.org/10.3390/ijms15034531.CrossRefPubMedPubMedCentralGoogle Scholar
  3. Chandler DJ, Waterhouse BD, Gao W-J. New perspectives on catecholaminergic regulation of executive circuits: evidence for independent modulation of prefrontal functions by midbrain dopaminergic and noradrenergic neurons. Front Neural Circuits. 2014;8:53.  https://doi.org/10.3389/fncir.2014.00053.CrossRefPubMedPubMedCentralGoogle Scholar
  4. Changeux JP, Edelstein SJ. Allosteric receptors after 30 years. Neuron. 1998;21:959–80.  https://doi.org/10.1016/S0896-6273(00)80616-9.CrossRefPubMedPubMedCentralGoogle Scholar
  5. Chatzidaki A, Millar NS. Allosteric modulation of nicotinic acetylcholine receptors. Biochem Pharmacol. 2015;97:408–17.  https://doi.org/10.1016/j.bcp.2015.07.028.CrossRefPubMedPubMedCentralGoogle Scholar
  6. Dani JA, Bertrand D. Nicotinic acetylcholine receptors and nicotinic cholinergic mechanisms of the central nervous system. Annu Rev Pharmacol Toxicol. 2007;47:699–729.  https://doi.org/10.1146/annurev.pharmtox.47.120505.105214.CrossRefPubMedPubMedCentralGoogle Scholar
  7. Fasoli F, Gotti C. Structure of neuronal nicotinic receptors. Curr Top Behav Neurosci. 2015;23:1–17.  https://doi.org/10.1007/978-3-319-13665-3_1.CrossRefPubMedPubMedCentralGoogle Scholar
  8. Gotti C, Clementi F. Neuronal nicotinic receptors: from structure to pathology. Prog Neurobiol. 2004;74:363–96.  https://doi.org/10.1016/j.pneurobio.2004.09.006.CrossRefPubMedPubMedCentralGoogle Scholar
  9. Hopur52009. Nicotinic_receptors.Png. Accessed on 27 July 2016, cited 27 July 2015. Available from: http://upload.wikimedia.org/wikipedia/commons/f/f1/Nicotinic_receptors.png
  10. Hurst R, Rollema H, Bertrand D. Nicotinic acetylcholine receptors: from basic science to therapeutics. Pharmacol Ther. 2013;137:22–54.  https://doi.org/10.1016/j.pharmthera.2012.08.012.CrossRefPubMedPubMedCentralGoogle Scholar
  11. Martindale R, Lester RAJ. On the discovery of the nicotinic acetylcholine receptor channel. In: Lester AJR, editor. Nicotinic receptors. New York: Springer; 2014. p. 1–16.Google Scholar
  12. Nakayama H, Shimoke K, Isosaki M, Satoh H, Yoshizumi M, Ikeuchi T. Subtypes of neuronal nicotinic acetylcholine receptors involved in nicotine-induced phosphorylation of extracellular signal-regulated protein kinase in PC12h cells. Neurosci Lett. 2006;392:101–4.  https://doi.org/10.1016/j.neulet.2005.09.003.CrossRefPubMedPubMedCentralGoogle Scholar
  13. Obeso JA, Rodriguez-Oroz MC, Benitez-Temino B, Blesa FJ, Guridi J, Marin C, et al. Functional organization of the basal ganglia: therapeutic implications for Parkinson’s disease. Mov Disord. 2008;23(Suppl 3):S548–59.  https://doi.org/10.1002/mds.22062.CrossRefPubMedPubMedCentralGoogle Scholar
  14. Picciotto MR, Brunzell DH, Caldarone BJ. Effect of nicotine and nicotinic receptors on anxiety and depression. Neuroreport. 2002;13:1097–106.PubMedCrossRefGoogle Scholar
  15. Pomerleau OF. Nicotine and the central nervous system: biobehavioral effects of cigarette smoking. Am J Med. 1992;93:2S–7S.PubMedCrossRefGoogle Scholar
  16. Rahman S. Nicotinic receptors as therapeutic targets for drug addictive disorders. CNS Neurol Disord Drug Targets. 2013;12:633–40.PubMedCrossRefGoogle Scholar
  17. Sarter M, Nelson CL, Bruno JP. Cortical cholinergic transmission and cortical information processing in schizophrenia. Schizophr Bull. 2005;31:117–38.  https://doi.org/10.1093/schbul/sbi006.CrossRefPubMedPubMedCentralGoogle Scholar
  18. Schaaf CP. Nicotinic acetylcholine receptors in human genetic disease. Genet Med. 2014;16:649–56.  https://doi.org/10.1038/gim.2014.9.CrossRefPubMedPubMedCentralGoogle Scholar
  19. Servier. Receptors and channels. Accessed on 27 July 2016, cited 27 July 2016. Available from: http://www.servier.com/slidekit/?item=5
  20. Taly A, Corringer PJ, Guedin D, Lestage P, Changeux JP. Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system. Nat Rev Drug Discov. 2009;8:733–50.  https://doi.org/10.1038/nrd2927.CrossRefPubMedGoogle Scholar

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© Springer International Publishing AG 2018

Authors and Affiliations

  • Josephine R. Tarren
    • 1
  • Joan Y. Holgate
    • 1
  • Selena E. Bartlett
    • 2
    Email author
  1. 1.Queensland University of TechnologyBrisbaneAustralia
  2. 2.Queensland University of Technology (QUT)BrisbaneAustralia