Table 1. Functional efficacy at recombinant human α7 nACh and 5-HT3A receptors determined by Ca2+ flux (FLIPR) assays.
| Agent | HEK293/Human α7 nAChR Mean ± SD EC50 (nM) | HEK293/Human 5-HT3A Mean ± SD IC50 (nM) | Ratio |
|---|---|---|---|
| BMS-933043 | 23.4 ± 10.6 (n = 16) | 8,066 ± 2,306 (n = 10) | 345 |
| EVP-6124 | 14.7 ± 11 (n = 4) | 4.0 ± 2.1 (n = 5) | 0.3 |
| TC-5619 | 3.9 ± 1.9 (n = 5) | >100,000 (n = 9) | >25,641 |
| A-582941 | 89.8 ± 54.3 (n = 6) | 102 ± 86 (n = 10) | 1.1 |
| PNU-282987 | 94.5 ± 27 (n = 9) | 24,920 ± 12,050 (n = 5) | 264 |
| NS-6740 | >100,000 (n = 7) | 4,827 ± 1,316 (n = 9) | Not calculated |