48
Views
17
CrossRef citations to date
0
Altmetric
Review

Neuronal nicotinic acetylcholine receptor ligands as potential analgesics

&
Pages 1003-1021 | Published online: 02 Mar 2005
 

Abstract

Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand-gated cation channels that mediate fast responses of neurons to the neurotransmitter acetylcholine (ACh). Although related to muscle nAChRs, neuronal nAChRs display a different pharmacology. Neuronal nAChR-mediated analgesia is observed in rodent pain models but activation of nAChRs can also produce undesirable effects, many related to autonomic function. However, nAChR subtype diversity provides the opportunity to develop selective agents with improved safety margins, with the α4β2 nAChR subtype important in attenuating acute thermal pain and the α3β4 subtype critical for autonomic function. Recent evidence that α7 nAChRs are involved in pain and inflammation is exciting but requires validation. Recent patent literature reveals increased interest in nAChR ligands for pain, as well as other therapeutic indications. New structure types are being developed, with new α7 ligands being particularly noteworthy but the minimal disclosure of biological data in many recent patents makes evaluation of their utility difficult.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.