Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.
A total of 20 substituted analogues of nicotine (1a) and homoazanicotine (3a) were examined in order to determine whether or not they might bind in a similar manner at alpha4beta2 nicotinic acetylcholinergic (nACh) receptors. It was found that parallel structural changes in the two series resulted in parallel shifts in affinity. Evidence suggests that the two series are binding in a comparable fashion.
Ferretti
G
G
Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA 23298, USA.
Dukat
M
M
Giannella
M
M
Piergentili
A
A
Pigini
M
M
Quaglia
W
W
Damaj
M I
MI
Martin
B R
BR
Glennon
R A
RA
D006801:Humans; D018716:Molecular Mimicry; D009474:Neurons / Q000737:chemistry; D009538:Nicotine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D011978:Receptors, Nicotinic / Q000378:metabolism*; D013329:Structure-Activity Relationship
D011978:Receptors, Nicotinic; C467228:homoazanicotine; D009538:Nicotine