Table 1

Comparison of the pharmacological potencies of nicotinic ligands in the tail-flick test after s.c. and i.t. administration to their binding affinities to [3H]-nicotine-labeled sites in the brain

DrugBrainKi (nM)ED50 s.c. (μmol/kg)ED50 i.t. (nmol/mouse)
(−)-Epibatidine0.050.0300.47
(+)-Epibatidine0.0450.0330.67
6-Chloronicotine0.631-a 0.681-a 3.37
N-MCC0.1420% @ 3513.7
Lobeline4.422% @ 5923
(±)-Iso-nicotine12.01-b 27.71-b 43
AMP-ME28.31-c 81.21-c 48.5
(−)-Nicotine1.4874
N-MNP181-c 951-c 80
(±)-nor-Nicotine2556146
(+)-Nicotine3154.3159
AMP-MP11401-c 11% @ 295173
ABT-418614200
Anabasine5347.5216
DMPP243% @ 94236
(+)-BN>10,0007.13290
Cytisine0.1435% @ 4210% @ 1000
Cotinine>10,0005% @ 1002% @ 1000

  • ↵1-a Dukat et al., 1996.

  • ↵1-b Glassco et al., 1994b.

  • ↵1-c Damaj et al., 1996a.