TABLE 2

IC50 values (nM) for the inhibition of ACh-evoked responses by bath applications of agonists and partial agonists

(α4)3(β2)2(α4)2(β2)3(α4)2(β2)2α5α7
nM
Nicotine56 ± 1615 ± 517 ± 71000 ± 380
Cytisine27 ± 148 ± 53.2 ± 1.61200 ± 570
Varenicline2.8 ± 1.31.6 ± 0.53.3 ± 0.9334 ± 140
3-pyr-Cyt16,000 ± 12,000600 ± 5002300 ± 1000N.A.
GTS-211000 ± 400170 ± 1001300 ± 475*
S 2479536,000 ± 700053,000 ± 600015,000 ± 4000*
  • N.A., not available.

  • * Inhibition after a phase of potentiation.