Alpha-3 beta-4 nicotinic receptor

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

As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3)m4)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[edit]

Agonists[edit]

Antagonists[edit]

Competitive[edit]

3d structure of "compound 5" (Zaveri 2010). Ki, 508 nM at α3β4 nAChR
  • compound 5, highly selective over α4β2 and α7[7]

Noncompetitive[edit]

See also[edit]

References[edit]

  1. ^ Stauderman KA, Mahaffy LS, Akong M et al. (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. 
  2. ^ 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. 
  3. ^ "Heterogeneity of nicotinic receptor class and subunit mRNA expression among individual parasympathetic neurons from rat intracardiac ganglia". US National Library of Medicine. Retrieved 31 August 2013. 
  4. ^ "Structural and functional diversity of native brain neuronal nicotinic receptors.". US National Library of Medicine. Retrieved 31 August 2013. 
  5. ^ a b c d e f g h i Xiao Y, Meyer EL, Thompson JM, Surin A, Wroblewski J, Kellar KJ (August 1998). "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. PMID 9687574. 
  6. ^ Bencherif, M.; Schmitt, J. D.; Bhatti, B. S.; Crooks, P.; Caldwell, W. S.; Lovette, M. E.; Fowler, K.; Reeves, L.; Lippiello, P. M. (1998). "The heterocyclic substituted pyridine derivative (+/-)-2-(-3-pyridinyl)-1-azabicyclo2.2.2octane (RJR-2429): A selective ligand at nicotinic acetylcholine receptors". The Journal of pharmacology and experimental therapeutics 284 (3): 886–894. PMID 9495846.  edit
  7. ^ Zaveri NT (2011). "The nociceptin/orphanin FQ receptor (NOP) as a target for drug abuse medications". Curr Top Med Chem 11 (9): 1151–6. PMID 21050175. 
  8. ^ a b Hernandez SC, Bertolino M, Xiao Y, Pringle KE, Caruso FS, Kellar KJ (2000). "Dextromethorphan and its metabolite dextrorphan block alpha3beta4 neuronal nicotinic receptors". J. Pharmacol. Exp. Ther. 293 (3): 962–7. PMID 10869398. 
  9. ^ a b Damaj MI, Flood P, Ho KK, May EL, Martin BR (February 2005). "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. doi:10.1124/jpet.104.075093. PMID 15356218. 
  10. ^ a b c "Blockade of Rat α3β4 Nicotinic Receptor Function by Methadone, Its Metabolites, and Structural Analogs — JPET". 
  11. ^ Arias HR, Targowska-Duda KM, Feuerbach D, Sullivan CJ, Maciejewski R, Jozwiak K (March 2010). "Different interaction between tricyclic antidepressants and mecamylamine with the human alpha3beta4 nicotinic acetylcholine receptor ion channel". Neurochem. Int. 56 (4): 642–9. doi:10.1016/j.neuint.2010.01.011. PMID 20117161. 
  12. ^ Miller, DK; Wong, EH; Chesnut, MD; Dwoskin, LP (Aug 2002). "Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors.". The Journal of pharmacology and experimental therapeutics 302 (2): 687–95. doi:10.1124/jpet.302.2.687. PMID 12130733. 
  13. ^ Toll, L.; Zaveri, N. T.; Polgar, W. E.; Jiang, F.; Khroyan, T. V.; Zhou, W.; Xie, X. (S.); Stauber, G. B.; Costello, M. R.; Leslie, F. M. (2012). "AT-1001: A High Affinity and Selective α3β4 Nicotinic Acetylcholine Receptor Antagonist Blocks Nicotine Self-Administration in Rats". Neuropsychopharmacology 37 (6): 1367–1376. doi:10.1038/npp.2011.322. PMC 3327842. PMID 22278092.  edit