TABLE 1

Functional potency and efficacy values for varenicline at rat neuronal nAChRs

EC50 values were determined from the fit data in Figs. 2C, 3C, and 4B. Efficacy values are presented as the percentage of maximum ACh response (see Materials and Methods). Efficacy values for α4β2, α3β4, and α7 are taken from the fit data in Figs. 2C, 3C, and 4B, respectively. Efficacy values for α3β2 and α6/α3β2β3 are derived from a single concentration of varenicline (100 μM). All values are presented as mean ± S.E.M.


Receptor

EC50

nH

Efficacy
μM %
α4β2 2.3 ± 0.3 1.1 ± 0.1 13.4 ± 0.4
α3β4 55 ± 8 2.0 ± 0.5 75 ± 6
α3β2 N.D. N.D. 3.7 ± 0.4
α6/α3β2β3 N.D. N.D. 8.8 ± 1.4
α7
18 ± 6
1.0 ± 0.3
93 ± 7
  • N.D., not determined.