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. Author manuscript; available in PMC: 2018 Jul 1.
Published in final edited form as: Bioorg Med Chem Lett. 2017 May 6;27(13):2990–2995. doi: 10.1016/j.bmcl.2017.05.014

Table 3.

Structures and activities for M4 PAM analogs 17.

graphic file with name nihms877330u4.jpg
Cmpd R hM4 EC50 (nM)a [% ACh Max ±SEM] hM4 pEC50 (±SEM)
17a graphic file with name nihms877330t18.jpg 25 [85±8] 7.61±0.08
17b graphic file with name nihms877330t19.jpg 28 [82±9] 7.56±0.03
17c graphic file with name nihms877330t20.jpg 282 [77±8] 6.55±0.04
17d graphic file with name nihms877330t21.jpg 141 [77±11] 6.88±0.11
17e graphic file with name nihms877330t22.jpg 1289 [81±8] 5.90±0.06
17f graphic file with name nihms877330t23.jpg 934 [86±1] 6.03±0.04
17g graphic file with name nihms877330t24.jpg 325 [75±13] 6.63±0.29
17h graphic file with name nihms877330t25.jpg 37 [94±9] 7.49±0.12
17i graphic file with name nihms877330t26.jpg 30 [84±5] 7.54±0.06
17j graphic file with name nihms877330t27.jpg 19 [88±5] 7.73±0.06
a

Calcium mobilization assays with hM4/Gqi5-CHO cells performed in the presence of an EC20 fixed concentration of acetylcholine; values represent means from three (n=3) independent experiments performed in triplicate.