Table 1.
Functional inhibition of calcium channels by compounds 3, 5a–c, 6a–c.
| Compound | logIC50 | SEM | IC50 (µM) | 95% CI (µM) |
|---|---|---|---|---|
| 3 a | ~–2.84 | 0.29 | 1452 b | 380–5550 |
| 5a | –4.34 | 0.01 | 46 | 44–48 |
| 6a | –3.90 | 0.03 | 124 c | 107–150 |
| 5b | –4.45 | 0.01 | 35 | 33–37 |
| 6b | –3.73 | 0.02 | 185 | 169–203 |
| 5c | ~–3.12 | 0.06 | 764 d | 575–1020 |
| 6c | –3.14 | 0.10 | 723 e | 447–1170 |
a This compound gave an IC50 of 6 µM in a radioligand displacement assay with 125I-GVIA [25] but it has since been established that it is less potent in an assay of functional activity at Cav2.2. [29]; b% Max inhibition, 15% at 300 µM; c% Max inhibition, 65% at 300 µM; d% Max inhibition, 30% at 300 µM; e% Max inhibition, 19% at 300 µM.