TABLE 1

Activation and Inhibition of α4β2 AChRs in an HEK cell line

Receptors Nicotine Acetylcholine DMPP Cytisine MCC DHβE Mecamylamine
Control nM
   Inhibition IC50 α4β2 6.1 ± 3.6 88 ± 24 770 ± 220
   Activation EC50 (α4)2(β2)3 116 ± 15 230 ± 40 1110 ± 550 57 ± 20 3200 ± 1000 >1,000,000
(α4)3(β2)2 2700 ± 200 57,000 ± 20,000
Nicotine-treated
   Activation EC50 (α4)2(β2)3 345 ± 40 320 ± 10 1320 ± 190 >1,000,000
(α4)3(β2)2 71,000 ± 37,000