Elsevier

Neuroscience Letters

Volume 213, Issue 3, 9 August 1996, Pages 201-204
Neuroscience Letters

An evaluation of neuronal nicotinic acetylcholine receptor activation by quaternary nitrogen compounds indicates that choline is selective for the α7 subtype

https://doi.org/10.1016/0304-3940(96)12889-5Get rights and content

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.

References (18)

There are more references available in the full text version of this article.

Cited by (255)

View all citing articles on Scopus
View full text