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. Author manuscript; available in PMC: 2014 Oct 10.
Published in final edited form as: J Med Chem. 2013 Sep 19;56(19):10.1021/jm401184f. doi: 10.1021/jm401184f

Table 2.

Inhibition in vitro binding affinities (Ki, nM) of the new series 7a–e, 10, 11, 14 and 15 and reference compounds toward α7-nAChR, heteromeric nAChR subtypes and 5-HT3.

Compound α7-nAChRa Heteromeric nAChR subtypes b 5-HT3 c Selectivity
α2β2 α2β4 α3β2 α3β4 α4β2 α4β4 α7/α4β2 α7/5HT3
7a 0.37, 0.45 >10000 4000 1000 709 562 1000 230 1370 561
7b 1.02, 1.37 ntd nt nt nt nt nt nt - -
7c 1.32, 1.35 1000 8000 2000 5000 885 3000 505 663 378
7d 1.83, 2.45 292 838 678 3000 141 1000 nt 66 -
7e 17.8, 20.3 >10000 562 2000 261 4000 251 nt 210 -
10 0.34, 0.35 nt nt nt nt nt nt nt - -
11 3.41, 6.21 nt nt nt nt nt nt nt - -
14 0.93, 1.93 nt nt nt nt nt nt nt - -
15 6.46, 8.77 784 6000 1000 9000 477 5000 nt 63 -
a

Rat cortical membranes, radiotracer [125I]α-bungarotoxin (0.1 nM), KD = 0.7 nM

b

Inhibition in vitro binding assay of all heteromeric nAChR subtypes was performed with stably transfected HEK293 cells and [3H]epibatidine (0.5 nM), KD = 0.021 nM (α2β2-nAChR), KD = 0.084 nM (α2β4-nAChR), KD = 0.034 nM (α3β2-nAChR), KD = 0.29 nM (α3β4-nAChR), KD = 0.046 nM (α4β2-nAChR), KD = 0.094 nM (α4β4-nAChR).55

c

Human 5-HT3 recombinant/HEK293 cells, radiotracer [3H]GR65630 (0.35 nM), KD = 0.5 nM

d

nt = not tested