Selective Agonists and Antagonists of α9 Versus α7 Nicotinic Acetylcholine Receptors.

ABSTRACT: Nicotinic acetylcholine receptors containing α9 subunits are essential for the auditory function and have been implicated, along with α7-containing nicotinic receptors, as potential targets for the treatment of inflammatory and neuropathic pain. The study of α9-containing receptors has been hampered by the lack of selective agonists. The only α9-selective antagonists previously identified are peptide conotoxins. Curiously, the activity of α7 and α9 receptors as modulators of inflammatory pain appears to not rely strictly on ion channel activation, which led to the identification of α7 "silent agonists" and phosphocholine as an "unconventional agonist" for α9 containing receptors. The parallel testing of the α7 silent agonist p-CF₃-diEPP and phosphocholine led to the disco

SUBMITTER: Papke RL 

PROVIDER: S-EPMC9547379 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature