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Alpha-3 beta-4 nicotinic receptor

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, is a type of nicotinic acetylcholine receptor, consisting of α3 and β4 subunits. It is located in the autonomic ganglia and adrenal medulla, where activation yields post- and/or presynaptic excitation, 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, making α3β4 a promising target for the development of novel antiaddictive agents.

Ligands

Source:

Agonists

  • Acetylcholine (endogenous neurotransmitter that binds non-selectively to nAChRs and mAChRs)
  • Anabaseine and other structural analogs
  • Carbachol
  • Cytisine (partial agonist)
  • Dimethylphenylpiperazinium
  • Epibatidine
  • Lobeline
  • Nicotine
  • RJR-2429

Antagonists

Competitive

3d structure of &quot;compound 5&quot; (Zaveri 2010). ''K''<sub>i</sub>, 508 nM at α<sub>3</sub>β<sub>4</sub> nAChR
  • DHβE
  • SR 16584, highly selective over α4β2 and α7

Noncompetitive

  • Dextromethorphan
  • Dextrorphan
  • Dextropropoxyphene
  • Hexamethonium
  • Imipramine
  • Levacetylmethadol
  • Mecamylamine
  • Methadone
  • Tubocurarine
  • Bupropion
  • Reboxetine
  • Ibogaine
  • Voacangine
  • 18-MC
  • 18-MAC
  • ME-18-MC
  • AT-1001
  • Choline

References

References

  1. Pharmacology, (Rang, Dale, Ritter & Moore, {{ISBN. 0-443-07145-4, 5th ed., Churchill Livingstone 2003) p. 138.
  2. (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.
  3. (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.
  4. (January 1997). "Heterogeneity of nicotinic receptor class and subunit mRNA expression among individual parasympathetic neurons from rat intracardiac ganglia". US National Library of Medicine.
  5. (October 2009). "Structural and functional diversity of native brain neuronal nicotinic receptors". US National Library of Medicine.
  6. (2015). "Role of β4* Nicotinic Acetylcholine Receptors in the Habenulo–Interpeduncular Pathway in Nicotine Reinforcement in Mice". Neuropsychopharmacology.
  7. (2023-08-01). "Advances in small molecule selective ligands for heteromeric nicotinic acetylcholine receptors". Pharmacological Research.
  8. (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.
  9. (January 2016). "Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype". European Journal of Medicinal Chemistry.
  10. (2004). "Antinociceptive effects of bethanechol or dimethylphenylpiperazinium in models of phasic or incisional pain in rats". Brain Res.
  11. Rang, H. P.. (2003). "Pharmacology". Churchill Livingstone.
  12. (March 1998). "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.
  13. "SR 16584 (CAS 1150153-86-8)".
  14. (2011). "The nociceptin/orphanin FQ receptor (NOP) as a target for drug abuse medications.". Current Topics in Medicinal Chemistry.
  15. (June 2000). "Dextromethorphan and its metabolite dextrorphan block alpha3beta4 neuronal nicotinic receptors". The Journal of Pharmacology and Experimental Therapeutics.
  16. (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.
  17. (October 2001). "Blockade of Rat α3β4 Nicotinic Receptor Function by Methadone, Its Metabolites, and Structural Analogs — JPET". Journal of Pharmacology and Experimental Therapeutics.
  18. (March 2010). "Different interaction between tricyclic antidepressants and mecamylamine with the human alpha3beta4 nicotinic acetylcholine receptor ion channel". Neurochemistry International.
  19. (August 2002). "Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors". The Journal of Pharmacology and Experimental Therapeutics.
  20. (May 2012). "AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats". Neuropsychopharmacology.
  21. (2004). "Cell Biology of the Chromaffin Cell". Instituto Teófilo Hernando.
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