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. 2016 Nov 6;173(24):3454–3466. doi: 10.1111/bph.13635

Table 1.

Published binding affinities and efficacies of nAChR ligands at α4β2 and α7 nAChRs

Drug K i (nM) α4β2 K i (nM) α7 Ratio α4β2/α7 % ACh at α4β2 % ACh at α7
Nicotine 3.5a 244a 70 40d 43d
(+/−)‐Epibatidine 0.026b 198b 7615 131d 150d
RTI‐36 0.037b >1000b >1000 ND ND
Varenicline 0.91c 37c 41 13d 74d
Cytisine 2.1c 228c 109 9c 83c
a

Grady et al. (2010).

b

Carroll et al. (2005).

c

Sala et al. (2013).

d

Ondachi et al. (2015).

ND, not determined.