Alpha-4 beta-2 nicotinic receptor
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Alpha-4 beta-2 nicotinic receptor
The alpha-4 beta-2 nicotinic receptor, also known as the α4β2 receptor, is a type of nicotinic acetylcholine receptor, consisting of α4 and β2 subunits.[1] It is located in the brain, where activation yields post- and presynaptic excitation[1], mainly by increased Na+ and K+ permeability.
The receptors exist in the two stoichiometries:
- (α4)2(β2)3 receptors have high sensitivity to nicotine and low Ca2+ permeability (HS receptors)
- (α4)3(β2)2 receptors have low sensitivity to nicotine and high Ca2+ permeability (LS receptors)
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Contents
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Ligands
Agonists
- Acetylcholine
- Cytisine
- Epibatidine
- Nicotine
- A-84,543
- A-366,833
- ABT-418
- Altinicline
- Dianicline
- Ispronicline
- Pozanicline
- Rivanicline
- Tebanicline
- TC-1827
- Varenicline
- Sazetidine A: full agonist on (α4)2(β2)3, 6% efficacy on (α4)3(β2)2[2]
- N-(3-pyridinyl)-bridged bicyclic diamines[3][4][5]
PAMs
- Desformylflustrabromine[6]
- Further compounds.. (see references →)[7][8]
Antagonists
- (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane[9]
- 2-fluoro-3-(4-nitro-phenyl)deschloroepibatidine[10]
- Coclaurine - alkaloid from Nelumbo nucifera[11]
- Mecamylamine[12]
- α-Conotoxin
- PNU-120,596
See also
References
- ^ a b Pharmacology, (Rang, Dale, Ritter & Moore, ISBN 0-443-07145-4, 5:th ed., Churchill Livingstone 2003) Page 138.
- ^ Zwart R, Carbone AL, Moroni M, et al. (2008). "Sazetidine-A is a potent and selective agonist at native and recombinant alpha 4 beta 2 nicotinic acetylcholine receptors". Mol. Pharmacol. 73 (6): 1838–43. doi:10.1124/mol.108.045104. PMID 18367540.
- ^ Bunnelle WH, Daanen JF, Ryther KB, et al. (2007). "Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors". J. Med. Chem. 50 (15): 3627–44. doi:10.1021/jm070018l. PMID 17585748.
- ^ Frost JM, Bunnelle WH, Tietje KR, et al. (2006). "Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists". J. Med. Chem. 49 (26): 7843–53. doi:10.1021/jm060846z. PMID 17181167.
- ^ Ji J, Schrimpf MR, Sippy KB, et al. (2007). "Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists". J. Med. Chem. 50 (22): 5493–508. doi:10.1021/jm070755h. PMID 17929796.
- ^ Kim JS, Padnya A, Weltzin M, Edmonds BW, Schulte MK, Glennon RA (2007). "Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator". Bioorg. Med. Chem. Lett. 17 (17): 4855–60. doi:10.1016/j.bmcl.2007.06.047. PMID 17604168.
- ^ Albrecht BK, Berry V, Boezio AA, et al. (2008). "Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators". Bioorg. Med. Chem. Lett. 18 (19): 5209–12. doi:10.1016/j.bmcl.2008.08.080. PMID 18789861.
- ^ Springer SK, Woodin KS, Berry V, et al. (2008). "Synthesis and activity of substituted carbamates as potentiators of the alpha4beta2 nicotinic acetylcholine receptor". Bioorg. Med. Chem. Lett. 18 (20): 5643–7. doi:10.1016/j.bmcl.2008.08.092. PMID 18805006.
- ^ Gao Y, Kuwabara H, Spivak CE, et al. (2008). "Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties". J. Med. Chem. 51 (15): 4751–64. doi:10.1021/jm800323d. PMID 18605717.
- ^ Abdrakhmanova GR, Damaj MI, Carroll FI, Martin BR (2006). "2-Fluoro-3-(4-nitro-phenyl)deschloroepibatidine is a novel potent competitive antagonist of human neuronal alpha4beta2 nAChRs". Mol. Pharmacol. 69 (6): 1945–52. doi:10.1124/mol.105.021782. PMID 16505153.
- ^ Kashiwada Y, Aoshima A, Keshiro Y, Chen YP, Furukawa H, Itoigawa M, Fujioka T, Mihashi K, Cosentino LM, Morris-Natschke SL, Lee KH. Anti-HIV benzylisoquinoline alkaloids and flavonoids from the leaves of Nelumbo nucifera, and structure–activity correlations with related alkaloids. Bioorganic & Medicinal Chemistry. January 2005; 13(2):443-448. doi:10.1016/j.bmc.2004.10.020
- ^ Fedorov NB, Benson LC, Graef J, Lippiello PM, Bencherif M (February 2009). "Differential pharmacologies of mecamylamine enantiomers: positive allosteric modulation and noncompetitive inhibition". J. Pharmacol. Exp. Ther. 328 (2): 525–32. doi:10.1124/jpet.108.146910. PMID 18957576.
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