Alpha-3 beta-4 nicotinic receptor

The alpha-3 beta-4 nicotinic receptor, also known as the α3β4 receptor and the ganglion-type nicotinic receptor,[1] is a type of nicotinic acetylcholine receptor, consisting of α3 and β4 subunits.[2][3] It is located in the autonomic ganglia[4] and adrenal medulla,[5] where activation yields post- and/or presynaptic excitation,[3] mainly by increased Na+ and K+ permeability.

As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3)m(β4)n where m + n = 5]. The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries.

Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior,[6] making α3β4 a promising target for the development of novel antiaddictive agents.

  1. ^ Pharmacology, (Rang, Dale, Ritter & Moore, ISBN 0-443-07145-4, 5th ed., Churchill Livingstone 2003) p. 138.
  2. ^ Stauderman KA, Mahaffy LS, Akong M, Veliçelebi G, Chavez-Noriega LE, Crona JH, Johnson EC, Elliott KJ, Gillespie A, Reid RT, Adams P, Harpold MM, Corey-Naeve J (February 1998). "Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells". The Journal of Pharmacology and Experimental Therapeutics. 284 (2): 777–89. PMID 9454827.
  3. ^ a b Xiao Y, Kellar KJ (July 2004). "The comparative pharmacology and up-regulation of rat neuronal nicotinic receptor subtype binding sites stably expressed in transfected mammalian cells". The Journal of Pharmacology and Experimental Therapeutics. 310 (1): 98–107. doi:10.1124/jpet.104.066787. PMID 15016836. S2CID 23900581.
  4. ^ Poth K, Nutter TJ, Cuevas J, Parker MJ, Adams DJ, Luetje CW (January 1997). "Heterogeneity of nicotinic receptor class and subunit mRNA expression among individual parasympathetic neurons from rat intracardiac ganglia". The Journal of Neuroscience. 17 (2). US National Library of Medicine: 586–96. doi:10.1523/JNEUROSCI.17-02-00586.1997. PMC 6573231. PMID 8987781.
  5. ^ Gotti C, Clementi F, Fornari A, Gaimarri A, Guiducci S, Manfredi I, Moretti M, Pedrazzi P, Pucci L, Zoli M (October 2009). "Structural and functional diversity of native brain neuronal nicotinic receptors" (PDF). Biochemical Pharmacology. 78 (7). US National Library of Medicine: 703–11. doi:10.1016/j.bcp.2009.05.024. PMID 19481063.
  6. ^ HarringtonEtAl, L. (2015). "Role of β4* Nicotinic Acetylcholine Receptors in the Habenulo–Interpeduncular Pathway in Nicotine Reinforcement in Mice". Neuropsychopharmacology. 41 (7): 1790–1802. doi:10.1038/npp.2015.346. PMC 4869047. PMID 26585290.