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Methyllycaconitine analogues have mixed antagonist effects at nicotinic acetylcholine receptors

Barker, David; Lin, Diana S-H; Carland, Jane E; Chu, Cindy P-Y; Chebib, Mary; Brimble, Margaret A; Savage, G Paul; McLeod, Malcolm


Bicyclic analogues of methyllycaconitine (MLA), such as 12, have been synthesised that incorporate the C1-OMe substituent present in the natural product. Electrophysiology experiments using Xenopus oocytes expressing nicotinic acetylcholine receptors (nAChRs) were conducted on these analogues and a related tricyclic analogue 2. The most potent compound, 2, was an antagonist at all receptors studied but displayed different antagonist effects at each receptor subtype. This study more clearly...[Show more]

CollectionsANU Research Publications
Date published: 2005
Type: Journal article
Source: Bioorganic and Medicinal Chemistry
DOI: 10.1016/j.bmc.2005.04.054


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