Methyllycaconitine analogues have mixed antagonist effects at nicotinic acetylcholine receptors
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 defines the biological effects of MLA analogues at nAChRs and demonstrates that these analogues are not selective ligands for the α7 nAChR subtype.
Barker, David,Lin, Diana H.-S.,Carland, Jane E.,Chu, Cindy P.-Y.,Chebib, Mary,Brimble, Margaret A.,Savage, G. Paul,McLeod, Malcolm D.
Synthesis and bioactivities of novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
Novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives were synthesized and evaluated for their abilities to inhibit lipopolysaccharide (LPS)-stimulated production of TNF-alpha in rat whole blood. Several of these compounds exhibited potent inhibitory activity.
Titanium mediated cyclization of N-substituted di(β-carbethoxyethyl)amines: Preparation of 1-substituted-3-carbethoxy-4-piperidones
Dieckmann cyclisation of N-substituted di(β-carbethoxyethyl)amines with titanium tetrachloride in DCM in the presence of triethylamine leads to the formation of 3-carbethoxy-4-piperidones.
Deshmukh,Sampath Kumar,Rama Rao
p. 177 - 182
(2007/10/02)
More Articles about upstream products of 99329-51-8