Biology:Alpha-3 beta-4 nicotinic receptor

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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.

Ligands

Source:[7]

Agonists

Antagonists

Competitive

3d structure of "compound 5" (Zaveri 2010). Ki, 508 nM at α3β4 nAChR
  • DHβE[8]
  • SR 16584,[13] highly selective over α4β2 and α7[14]

Noncompetitive

See also

References

  1. ↑ Pharmacology, (Rang, Dale, Ritter & Moore, ISBN:0-443-07145-4, 5th ed., Churchill Livingstone 2003) p. 138.
  2. ↑ "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. February 1998. PMID 9454827. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=9454827. 
  3. ↑ 3.0 3.1 "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. July 2004. doi:10.1124/jpet.104.066787. PMID 15016836. 
  4. ↑ "Heterogeneity of nicotinic receptor class and subunit mRNA expression among individual parasympathetic neurons from rat intracardiac ganglia". The Journal of Neuroscience (US National Library of Medicine) 17 (2): 586–96. January 1997. doi:10.1523/JNEUROSCI.17-02-00586.1997. PMID 8987781. 
  5. ↑ "Structural and functional diversity of native brain neuronal nicotinic receptors". Biochemical Pharmacology (US National Library of Medicine) 78 (7): 703–11. October 2009. doi:10.1016/j.bcp.2009.05.024. PMID 19481063. https://hal.archives-ouvertes.fr/hal-00509504/file/PEER_stage2_10.1016%252Fj.bcp.2009.05.024.pdf. 
  6. ↑ HarringtonEtAl, L. (2015). "Role of β4* Nicotinic Acetylcholine Receptors in the Habenulo–Interpeduncular Pathway in Nicotine Reinforcement in Mice". Neuropsychopharmacology 41: 1790-1802. doi:10.1038/npp.2015.346. PMC 4869047. https://www.nature.com/articles/npp2015346#Abs1. Retrieved 8 February 2023. 
  7. ↑ Matera, Carlo; Papotto, Claudio; Dallanoce, Clelia; De Amici, Marco (2023-08-01). "Advances in small molecule selective ligands for heteromeric nicotinic acetylcholine receptors". Pharmacological Research 194: 106813. doi:10.1016/j.phrs.2023.106813. ISSN 1043-6618. https://www.sciencedirect.com/science/article/pii/S104366182300169X. 
  8. ↑ 8.0 8.1 8.2 8.3 8.4 8.5 8.6 8.7 8.8 "Rat alpha3/beta4 subtype of neuronal nicotinic acetylcholine receptor stably expressed in a transfected cell line: pharmacology of ligand binding and function". Molecular Pharmacology 54 (2): 322–33. August 1998. doi:10.1124/mol.54.2.322. PMID 9687574. 
  9. ↑ "Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype". European Journal of Medicinal Chemistry 108: 392–405. January 2016. doi:10.1016/j.ejmech.2015.11.045. PMID 26706350. 
  10. ↑ "Antinociceptive effects of bethanechol or dimethylphenylpiperazinium in models of phasic or incisional pain in rats". Brain Res 1018 (2): 272–82. 2004. doi:10.1016/j.brainres.2004.05.085. PMID 15276888. 
  11. ↑ Rang, H. P. (2003), Pharmacology, Edinburgh: Churchill Livingstone, ISBN 0-443-07145-4  Page 149
  12. ↑ "The heterocyclic substituted pyridine derivative (+/-)-2-(-3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429): a selective ligand at nicotinic acetylcholine receptors". The Journal of Pharmacology and Experimental Therapeutics 284 (3): 886–94. March 1998. PMID 9495846. 
  13. ↑ "SR 16584 (CAS 1150153-86-8)". https://www.rndsystems.com/products/sr-16584_4424. 
  14. ↑ Zaveri, NT (2011). "The nociceptin/orphanin FQ receptor (NOP) as a target for drug abuse medications.". Current Topics in Medicinal Chemistry 11 (9): 1151–6. doi:10.2174/156802611795371341. PMID 21050175. 
  15. ↑ 15.0 15.1 "Dextromethorphan and its metabolite dextrorphan block alpha3beta4 neuronal nicotinic receptors". The Journal of Pharmacology and Experimental Therapeutics 293 (3): 962–7. June 2000. PMID 10869398. 
  16. ↑ 16.0 16.1 "Effect of dextrometorphan and dextrorphan on nicotine and neuronal nicotinic receptors: in vitro and in vivo selectivity". The Journal of Pharmacology and Experimental Therapeutics 312 (2): 780–5. February 2005. doi:10.1124/jpet.104.075093. PMID 15356218. 
  17. ↑ 17.0 17.1 17.2 Xiao, Yingxian; Smith, Richard D.; Caruso, Frank S.; Kellar, Kenneth J. (October 2001). "Blockade of Rat α3β4 Nicotinic Receptor Function by Methadone, Its Metabolites, and Structural Analogs — JPET". Journal of Pharmacology and Experimental Therapeutics 299 (1): 366–371. http://jpet.aspetjournals.org/content/299/1/366.abstract. 
  18. ↑ "Different interaction between tricyclic antidepressants and mecamylamine with the human alpha3beta4 nicotinic acetylcholine receptor ion channel". Neurochemistry International 56 (4): 642–9. March 2010. doi:10.1016/j.neuint.2010.01.011. PMID 20117161. 
  19. ↑ "Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors". The Journal of Pharmacology and Experimental Therapeutics 302 (2): 687–95. August 2002. doi:10.1124/jpet.302.2.687. PMID 12130733. 
  20. ↑ "AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats". Neuropsychopharmacology 37 (6): 1367–76. May 2012. doi:10.1038/npp.2011.322. PMID 22278092. 
  21. ↑ "Choline as a tool to evaluate nicotinic receptor function in chromaffin cells". Cell Biology of the Chromaffin Cell. Spain: Instituto Teófilo Hernando. 2004. https://isccb12.webs.ull.es/PDF-Final/38-Rubio.pdf. 



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