Table 1

Inhibition of specific S-(−)-[3H]nicotine binding to rat striatal membranes by novelN-n-alkylnicotinium analogs: comparison with reference compounds DHβE, S-(−)-nicotine, andR-(+)-nicotine

Compoundn-Alkyl Chain LengthIC5095% CI1-aKi95% CISlope Factor1-bs.e.1-c
μM μM
NDNI100.230.20,  0.270.090.08,  0.11−0.9580.066
NDDNI120.350.28,  0.430.140.11,  0.17−0.8540.053
NHxNI61.321.15,  1.500.530.46,  0.60−0.9040.045
NNNI92.091.83,  2.390.840.73,  0.95−1.0640.045
NENI22.601.89,  3.581.040.76,  1.43−1.1060.179
NHpNI75.144.64,  5.702.061.85,  2.28−1.0310.027
NMNI18.826.94,  11.23.532.77,  4.48−0.9570.047
NnBNI427.224.2,  30.710.99.70,  12.3−1.1070.089
NPNI353.745.6,  63.421.518.2,  25.3−0.9360.076
NONI849.338.6,  62.919.715.4,  25.1−1.1360.112
DHβENA1-d 0.360.24,  0.530.140.09,  0.21−0.6670.067
S-(−)-Nicotine00.0020.001,  0.0040.00080.0007,  0.0040−0.8160.029
R-(+)-Nicotine00.120.10,  0.150.050.04,  0.06−0.9930.091

IC50 values were derived from variable-slope, sigmoid curve fits to the mean data from four to six independent observations.Ki values were derived from IC50values using the Cheng-Prusoff equation.

  • 1-a 95% CI = 95% confidence interval.

  • 1-b Pseudo-Hill coefficient, derived using a variable slope model.

  • 1-c s.e. = standard error of slope factor.

  • 1-d NA = not applicable.