Table 1. Structure and Activities of Analogs 13a.
| Compound | Ar | n | hM5 EC50 (nM) (pEC50±SEM) | hM5 % ACh Max |
|---|---|---|---|---|
| 8 |
|
1 | 481 (6.34±0.08) | 71±4 |
| 13a |
|
1 | 976 (6.05±0.13) | 80±5 |
| 13b |
|
1 | 672 (6.18±0.06) | 75±6 |
| 13c |
|
1 | 889 (6.07±0.10) | 79±6 |
| 13d |
|
1 | 2,216 (5.67±0.09) | 80±4 |
| 13e |
|
1 | 2,823 (5.56±0.06) | 68±3 |
| 13f |
|
1 | 606 (6.25±0.09) | 77±6 |
| 13g |
|
1 | 1,005 (6.00±0.02) | 73±5 |
| 13h |
|
1 | > 10,000 (<5) | <25 |
| 13i |
|
1 | 1,713 (5.80±0.12) | 74±4 |
| 13j |
|
1 | 5,102 (5.31±0.09) | 71±4 |
| 13k |
|
2 | 256 (6.59±0.03) | 74±3 |
| 13l |
|
2 | 255 (6.61±0.12) | 76±0 |
a
hM5 pEC50, and ACh Max data reported as averages ± SEM from our functional calcium assay; n = 3 determinations.