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. Author manuscript; available in PMC: 2019 Jul 18.
Published in final edited form as: ACS Chem Neurosci. 2018 Apr 26;9(7):1572–1581. doi: 10.1021/acschemneuro.8b00126

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
a

hMs and rMs pEC50 and ACh Max data reported as averages ± SEM from our functional calcium assay; n = 3 determinations.