A comparison of the binding of three series of nicotinic ligands.
A total of 24 aryl-substituted analogues of nicotine (1a) and two related series of nicotinic ligands, aminomethylpyridines 3 and ether analogues 8, were examined to determine if they bind at alpha4beta2 nACh receptors in a common manner. A modest correlation (r=0.785) was found between the affinities of the nicotine analogues and derivatives of 3, but little correlation (r=0.348) was found with analogues 8. However, a modest correlation (r=0.742) exists between the binding of analogues 3 and 8. It seems that 1-series and 8-series compounds bind differently but that the 3-series compounds share some intermediate binding similarity with both.
Lee
Mase
M
Department of Medicinal Chemistry, School of Pharmacy, Box 980540, Virginia Commonwealth University, Richmond 23298, USA.
Dukat
Malgorzata
M
Liao
Liang
L
Flammia
Dwight
D
Damaj
M Imad
MI
Martin
Billy
B
Glennon
Richard A
RA
D000818:Animals; D001921:Brain / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004986:Ether / Q000031:analogs & derivatives; D007546:Isoquinolines / Q000737:chemistry; D007700:Kinetics; D008024:Ligands; D009538:Nicotine / Q000031:analogs & derivatives* / Q000378:metabolism*; D011485:Protein Binding; D011725:Pyridines / Q000737:chemistry; D011869:Radioligand Assay; D051381:Rats; D011978:Receptors, Nicotinic / Q000378:metabolism*; D013223:Statistics as Topic; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D007546:Isoquinolines; D008024:Ligands; D011725:Pyridines; D011978:Receptors, Nicotinic; C403531:nicotinic receptor alpha4beta2; D004986:Ether; D009538:Nicotine