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, 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
- mAChRs)
- Anabaseine and other structural analogs[9]
- Carbachol[8]
- Cytisine (partial agonist) [8]
- Dimethylphenylpiperazinium[10]
- Epibatidine[8]
- Lobeline[11]
- Nicotine[8]
- RJR-2429[12]
Antagonists
Competitive
_with_tube_model.png)
Noncompetitive
- Dextromethorphan[15][16]
- Dextrorphan[15][16]
- Dextropropoxyphene[17]
- Hexamethonium[8]
- Imipramine[18]
- Levacetylmethadol[17]
- Mecamylamine[8]
- Methadone[17]
- Tubocurarine[8]
- Bupropion
- Reboxetine[19]
- Ibogaine
- Voacangine
- 18-MC
- 18-MAC
- ME-18-MC
- AT-1001[20]
- Choline[21]
See also
- α3β2-Nicotinic receptor
- α4β2-Nicotinic receptor
- α7-Nicotinic receptor
- Muscle-type nicotinic receptor
References
- ISBN 0-443-07145-4, 5th ed., Churchill Livingstone 2003) p. 138.
- PMID 9454827.
- ^ S2CID 23900581.
- PMID 8987781.
- PMID 19481063.
- PMID 26585290.
- ISSN 1043-6618.
- ^ PMID 9687574.
- PMID 26706350.
- S2CID 45145197.
- ISBN 0-443-07145-4Page 149
- PMID 9495846.
- ^ "SR 16584 (CAS 1150153-86-8)". R&D Systems. Retrieved 3 December 2017.
- PMID 21050175.
- ^ PMID 10869398.
- ^ S2CID 149958.
- ^ a b c 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.
- S2CID 29461221.
- PMID 12130733.
- PMID 22278092.
- ^ González-Rubioa JM, Rojoa J, Tapiaa L, Maneud V, Muletc J, Valorc LM, Criadoc M, Salac F, García AG, Gandía L (2004). "Choline as a tool to evaluate nicotinic receptor function in chromaffin cells" (PDF). In Borges R, Gandía L (eds.). Cell Biology of the Chromaffin Cell. Spain: Instituto Teófilo Hernando.