Table 5. Human and Rat M1 PAM Activities for Select Analogs 14–18.
Cpd | rat M1 PAM EC50 (μM)a [% ach Max ± SEM] | rat M1 pEC50 (±SEM) | hum M1 PAM EC50 (μM)a [% ACh max ± SEM] | hum M1 pEC50 (±SEM) |
---|---|---|---|---|
14a | 0.04, [87 ± 0] | 7.41 ± 0.06 | 0.06, [83 ± 3] | 7.22 ± 0.10 |
14c | 0.10, [90 ± 1] | 7.00 ± 0.03 | 0.09, [80 ± 8] | 7.05 ± 0.20 |
15a | 0.18, [87 ± 1] | 6.74 ± 0.03 | 0.18, [84 ± 2] | 6.74 ± 0.10 |
15b | 0.10, [87 ± 1] | 7.02 ± 0.04 | 0.12, [79 ± 4] | 6.91 ± 0.10 |
16 | 0.56, [89 ± 1] | 6.25 ± 0.05 | 0.66, [87 ± 3] | 6.18 ± 0.10 |
18c | 0.23, [93 ± 0] | 6.64 ± 0.07 | 0.32, [84 ± 7] | 6.49 ± 0.05 |
Calcium mobilization assays with rM1-CHO or hM1-CHO cells performed in the presence of an EC20 fixed concentration of acetylcholine for PAM; values represent means from three (n = 3) independent experiments performed in triplicate.