An evaluation of neuronal nicotinic acetylcholine receptor activation by quaternary nitrogen compounds indicates that choline is selective for the α7 subtype
Neuroscience LettersPublished 1 August 1996
Roger L. Papke, Merouane Bencherif, Patrick M. Lippiello
Citations274
SJR quartileQ2
SJR score0.77
SNIP0.67
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Abstract
The agonist properties of acetylcholine (ACh), tetramethylammonium, ethyl-trimethylammonium and choline were evaluated for muscle and neuronal nicotinic receptors in Xenopus oocytes. The only essential feature for a neuronal receptor agonist appears to be the charged nitrogen. For specific receptor subtypes, other structural elements appear permissive (neither increasing nor decreasing activity) or non-permissive (decreasing activity). Choline was a full agonist for α7, but a hydroxyl group was strongly non-permissive for other receptor subtypes (α1β1γδ, α3β2, and α4β2). The binding of these ligands to brain membranes is consistent with the electrophysiological results. Physiological concentrations of choline desensitize α7 receptors to ACh suggesting that, in vivo, choline may regulate both the activation and inactivation of this receptor.
Keywords
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