TABLE 1

The potency and efficacy of epibatidine at α4β2, α4β4, and α7 nAChRs stably expressed in mammalian cells are significantly increased by 2087101

Fluo-3-AM-loaded cells stably expressing human α3β4, α4β2, α4β4, and α7 nAChRs were challenged with epibatidine in the presence or absence of 1 μM 2087101 (α4β2, α4β4) or 3 μM 2087101 (α3β4, α7) as indicated. Cell population Ca2+ measurements were recorded using a FLIPR. Each value represents the mean ± S.E.M. from at least four independent experiments.


nAChR Subtype

Control

Treated with 2087101
EC50
Emax
EC50
Emax
nM % nM %
α3β4 11 ± 1 96 ± 2 11 ± 2* 101 ± 3*
α4β2 15.6 ± 1.5 103 ± 7 6.1 ± 1.1** 146 ± 6**
α4β4 3.8 ± 0.9 99 ± 6 0.9 ± 0.3*** 123 ± 5***
α7
79 ± 14
133 ± 9
38 ± 6***
187 ± 14**
  • * EC50 and Emax values for α3β4 were not statistically different between control and 2087101-treated cells.

  • ** p < 0.01.

  • *** p < 0.05.