Table 2. Displacement of [3H]-A-585539 binding to rat brain or recombinant human α7 nAChR.
Agent | Rat Brain α7 nAChR Mean ± SD Ki (nM) | HEK293/Human α7 nAChR Mean ± SD Ki (nM) |
---|---|---|
BMS-933043 | 3.3 ± 0.45 (n = 6) | 8.1 ± 1.96 (n = 4) |
Epibatidine | 5.2 ± 0.78 (n = 6) | 10.5 ± 1.58 (n = 4) |
TC-5619 | 0.23 ± 0.07 (n = 2) | 0.9 ± 0.14 (n = 2) |
EVP-6124 | 0.8 ± 0.33 (n = 2) | 3 ± 1.13 (n = 2) |
A-582941 | 21.7 ± 1.9 (n = 2) | 82.6 ± 14.3 (n = 3) |
MLA | 0.25 ± 0.07 (n = 2) | 4.17 ± 0.23 (n = 3) |
NS-6740 | 2.85 ± 0.44 (n = 3) | Not tested |
(-) Nicotine | 341 ± 69 (n = 2) | 526 ± 58 (n = 3) |