TABLE 1

Ki values for varenicline at α6β2* and α4β2* nAChRs in rat and monkey striatum

[125I]α-CtxMII competition studies were done in rat and monkey striatum to measure α6β2* nAChRs, whereas [125I]epibatidine binding in the presence of α-CtxMII was used to detect α4β2* nAChRs. Results show that varenicline potently interacts with both α6β2* and α4β2* nAChRs. Data with nicotine are provided for comparison. The values represent the mean ± S.E.M. of eight rats or three monkeys.

DrugAnimalKiRatio of Ki Values α6β2*/α4β2*
α6β2* nAChRsα4β2* nAChRs
nM
VareniclineRat0.12 ± 0.020.14 ± 0.010.86
Monkey0.13 ± 0.010.19 ± 0.110.68
NicotineRat1.68 ± 0.153.77 ± 0.760.46
Monkey0.61 ± 0.091.43 ± 0.240.43