Potencies and efficacies of ACh, GTS-21, and PNU-282987 on α7 currents in the absence or presence of test concentrations of PAMs
Test Concentration | Acetylcholine | GTS-21 | PNU-282987 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| pEC50 | Max | Hill Slope | pEC50 | Max | Hill Slope | pEC50 | Max | Hill Slope | ||||||||
| μM | % | % | % | |||||||||||||
| 3.9 ± 0.05 | 101 ± 4.3 | 1.6 | <4.0 | —a | 5.6 ± 0.12 | 77 ± 5.6 | 1.1 | |||||||||
| 5-HI | 1000 | 4.2 ± 0.04 | 206 ± 5.5 | 1.6 | 4.8 ± 0.04 | 81 ± 2.4 | 1.9 | 6.3 ± 0.05 | 155 ± 4.8 | 1.5 | ||||||
| Genistein | 50 | 4.3 ± 0.05 | 167 ± 5.1 | 1.6 | 4.6 ± 0.11 | 67 ± 6.9 | 1.4 | 6.3 ± 0.04 | 105 ± 2.7 | 1.7 | ||||||
| PNU-120596 | 3 | 4.8 ± 0.04 | 331 ± 8.9 | 2.8 | 5.1 ± 0.03 | 167 ± 7.1 | 2.9 | 6.7 ± 0.07 | 188 ± 8.3 | 2.1 | ||||||
| TQS | 5 | 4.7 ± 0.04 | 151 ± 3.3 | 1.8 | 5.0 ± 0.04 | 106 ± 8.4 | 2.9 | 6.7 ± 0.25 | 155 ± 22.1 | 1.7 | ||||||
↵ a At the highest tested concentration, 300 μM, the response was 26.5 ± 3.9%. The n values are 3 to 9.