Table 3. Agonist efficacy of BMS-933043, EVP-6124 and TC-5619 determined by patch clamp electrophysiology at recombinant human and rat α7 nAChRs expressed in HEK293 cells.
Agent | Species | Mean ± SEM Peak Current Ymaxobs @ 10 μM | Mean ± SEM Net Charge Ymax | Mean ± SEM Net Charge EC50 (μM) |
---|---|---|---|---|
BMS-933043 | Human (n = 7) | 0.24 ± 0.03 | 0.78 ± 0.004 | 0.29 ± 0.01 |
Rat (n = 4) | 0.27 ± 0.02 | 0.67 ± 0.07 | 0.14 ± 0.03 | |
EVP-6124 | Human (n = 4) | 0.32 ± 0.05 | 1.36 ± 0.09 | 0.07 ± 0.02 |
TC-5619 | Rat (n = 3) | 0.55 ± 0.06 | 1.26 ± 0.02 | 0.08 ± 0.01 |