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. 2018 Sep 4;9(9):917–922. doi: 10.1021/acsmedchemlett.8b00261

Table 5. Human and Rat M1 PAM Activities for Select Analogs 1418.

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
a

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.