Alpha-4 beta-2 nicotinic receptor

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The alpha-4 beta-2 nicotinic receptor ((α4)2(β2)3) is a type of nicotinic acetylcholine receptor, consisting of α4 and β2 subunits1.

It is located in the brain, where activation yields post- and presynaptic excitation1, mainly by increased Na+ and K+ permeability.

Contents

Agonists

Nicotinic agonists for this receptor include:

PAMs

Antagonists

  • (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane8
  • 2-fluoro-3-(4-nitro-phenyl)deschloroepibatidine9
  • mecamylamine
  • α-conotoxin

References

  1. ^ a b Pharmacology, (Rang, Dale, Ritter & Moore, ISBN 0443071454, 5:th ed., Churchill Livingstone 2003) Page 138.
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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. 
  9. ^ 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. 
v • d • e
Ion channel, receptor: ligand-gated ion channels
Cys-loop receptors
5-HT3 (A, B, C, D, E)
GABA A (α1, α2, α3, α4, α5, α6, β1, β2, β3, γ1, γ2, γ3, δ, ε, π, θ) • GABA C (ρ1, ρ2, ρ3)
α1 • α2 • α3 • α4 • β
monomers: α1 • α2 • α3 • α4 • α5 • α6 • α7 • α9 • α10 • β1 • β2 • β3 • β4 • δ • ε
pentamers: (α4)2(β2)3 • (α7)5 • (α1)2(β4)3 - Ganglion type • (α1)2β1δε - Muscle type
Ionotropic glutamates
AMPA (1, 2, 3, 4) • Kainate (1, 2, 3, 4, 5)  • NMDA (1, 2A, 2B, 2C, 2D, 3A, 3B, L1A, L1B)
ATP-gated channels

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