TABLE 2

The effects of cytisine and derivates on neuronal nAChR expressed in Xenopus oocytes

SpeciesReceptorEC50IC50ImaxRef.
μM
Cytisine
    Ratα4β2≈30.14Papke and Heinemann, 1994
    HumanHS α4β2<0.05Mineur et al., 2009
    Mouseα4β2(HS)120.08
    HumanLS α4β2130.1Mineur et al., 2009
    Mouseα4β2(LS)130.04
    Ratα3β4N.D.2≥1.0Papke and Heinemann, 1994
    Mouseα3β4201.0
    Ratα3β20.025Papke and Heinemann, 1994
    Mouseα3β2<0.02
    Ratα7130.73Papke and Papke, 2002
    Humanα7140.90Papke and Papke, 2002
    Mouseα7701.0
Varenicline
    Ratα4β22.20.13Mihalak et al., 2006
    HumanHS α4β20.10.13
    HumanLS α4β260.08
    Mouseα4β22.60.11
    Ratα3β4550.75Mihalak et al., 2006
    Mouseα3β4370.58
    Ratα3β2<0.10Mihalak et al., 2006
    Mouseα3β2<0.03
    Ratα71830.93Mihalak et al., 2006
    Humanα72.41.2
    Mouseα70.81.0
3-pyr-Cyt
    HumanHS α4β2120.08Mineur et al., 2009
    HumanLS α4β2310.03Mineur et al., 2009
    Mouseα4β2<0.01
    Mouseα3β4<0.01
    Mouseα3β2<0.01
    Humanα7>100≈0.20Mineur et al., 2009
    Mouseα7>3000≈0.94
Inhibition by 3-pyr-Cyt
    Humanα4β260Mineur et al., 2009
    Mouseα4β210

  • Data without specific references were obtained as part of the current study.

  • ↵1 The designations HS α4β2 and LS α4β2 indicate receptors with defined subunit composition formed by the coexpression of either α4 or β2 with linked α4 β2 concatamers. The designations α4β2(HS) and α4β2(LS) indicate that data were obtain from a mixed receptor populations that were best-fit with a two-site model.

  • ↵2 Not determined, because a full concentration-response study was not conducted.

  • ↵3 Likely an underestimate of potency because data are based on peak current rather than net charge.

  • ↵4 Estimated as described previously (Papke, 2006).