Table 4.
Human and Rat M5 PAM Activities of Select Analogs 18a
| compd | hM5 EC50 (nM) (pEC50 ± SEM) | hM5 % ACh Max | rM5 EC50 (nM) (pEC50 ± SEM) | rM5 % ACh Max |
|---|---|---|---|---|
| 18a | 500 (6.42 ± 0.26) | 83 ± 5 | 418 (6.40 ± 0.10) | 82 ± 4 |
| 18g | 41 (7.46 ± 0.15) | 74 ± 6 | 74 (7.13 ± 0.04) | 76 ± 7 |
| 18h | 58 (7.35 ± 0.13) | 72 ± 7 | 79 (7.12 ± 0.07) | 84 ± 2 |
| 18i | 76 (7.20 ± 0.12) | 79 ± 6 | 71 (7.19 ± 0.14) | 75 ± 8 |
| 18j | 161 (6.86 ± 0.11) | 76 ± 6 | 196 (6.71 ± 0.02) | 81 ± 3 |
hMs and rMs pEC50 and ACh Max data reported as averages ± SEM from our functional calcium assay; n = 3 determinations.