Methyllycaconitine analogues have mixed antagonist effects at nicotinic acetylcholine receptors

…, JE Carland, CPY Chu, M Chebib, MA Brimble…

Index: Barker, David; Lin, Diana H.-S.; Carland, Jane E.; Chu, Cindy P.-Y.; Chebib, Mary; Brimble, Margaret A.; Savage, G. Paul; McLeod, Malcolm D. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 14 p. 4565 - 4575

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Citation Number: 54

Abstract

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 ...

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