TABLE 1

Activation and inhibition parameters for benzylidene anabaseines

Name
R1
R2
R3
Imax
EC50
IC50
Ratio
BAa H H H 0.11 40 108 2.7
2,4DiMeOBAb OCH3 OCH3 H 0.10 11 25 2.3
2,4DiOHBAc OH OH H 0.47 2.9 >2000 >1000
4OH2MeOBAb OH OCH3 H 0.37 4.5 1140 253
2OH4MeOBAc OCH3 OH H 0.55 2.4 971 404
4MeS-BAa SCH3 H H 0.11 85 342 4.0
4OH-BAa OH H H 0.29 3.5 171 49
4AminoBA NH2 H H 0.5 3.7 334 90
4MeOBA OCH3 H H 0.34 15 71 4.7
4MeBA CH3 H H 0.13 76 216 2.8
2MeBA H CH3 H 0.07 32 >1000 >100
3MeBA H H CH3 0.17 240 103 0.43
3CNBA H H CN 0.06 >100 1400 ≈5
3NitroBA H H NO2 0.1 >100 750 ≈2.5
3OHBA H H OH 0.66 6.3 146 23
3MeOBA H H OCH3 0.19 50 125 2.5
2MeOBA
H
OCH3
H
0.15
26
360
14

  • ↵ a Data taken from Papke et al. (2004a)

  • ↵ b Data taken from Papke and Papke (2002)

  • ↵ c Data taken from Kem et al. (2004)