Are alpha9alpha10 nicotinic acetylcholine receptors a pain target for alpha-conotoxins?

Nevin, S, Clark, R, Klimis, H, Christie, M, Craik, D and Adams, DJ 2007, 'Are alpha9alpha10 nicotinic acetylcholine receptors a pain target for alpha-conotoxins?', Molecular Pharmacology, vol. 72, no. 6, pp. 1406-1410.


Document type: Journal Article
Collection: Journal Articles

Title Are alpha9alpha10 nicotinic acetylcholine receptors a pain target for alpha-conotoxins?
Author(s) Nevin, S
Clark, R
Klimis, H
Christie, M
Craik, D
Adams, DJ
Year 2007
Journal name Molecular Pharmacology
Volume number 72
Issue number 6
Start page 1406
End page 1410
Total pages 4
Publisher American Society for Pharmacology and Experimental Therapeutics
Abstract The synthetic alpha-conotoxin Vc1.1 is a small disulfide bonded peptide currently in development as a treatment for neuropathic pain. Unlike Vc1.1, the native post-translationally modified peptide vc1a does not act as an analgesic in vivo in rat models of neuropathic pain. It has recently been proposed that the primary target of Vc1.1 is the alpha9alpha10 nicotinic acetylcholine receptor (nAChR). We show that Vc1.1 and its post-translationally modified analogs vc1a, [P6O]Vc1.1, and [E14?]Vc1.1 are equally potent at inhibiting ACh-evoked currents mediated by alpha9alpha10 nAChRs. This suggests that alpha9alpha10 nAChRs are unlikely to be the molecular mechanism or therapeutic target of Vc1.1 for the treatment of neuropathic pain.
Subject Basic Pharmacology
DOI - identifier 10.1124/mol.107.040568
Copyright notice © 2007 The American Society for Pharmacology and Experimental Therapeutics
ISSN 0026-895X
Versions
Version Filter Type
Citation counts: Scopus Citation Count Cited 69 times in Scopus Article | Citations
Altmetric details:
Access Statistics: 189 Abstract Views  -  Detailed Statistics
Created: Mon, 28 Jun 2010, 10:15:46 EST by Catalyst Administrator
© 2014 RMIT Research Repository • Powered by Fez SoftwareContact us