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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 2.

Structures and activities for M4 PAM analogs 16.

graphic file with name nihms877330u3.jpg
Cmpd R hM4 EC50 (nM)a [% ACh Max ±SEM] hM4 pEC50 (±SEM)
16a graphic file with name nihms877330t1.jpg 439 [87±4] 6.36±0.04
16b graphic file with name nihms877330t2.jpg 419 [89±6] 6.45±0.19
16c graphic file with name nihms877330t3.jpg 106 [81±4] 7.04±0.16
16d graphic file with name nihms877330t4.jpg 124 [81±9] 6.99±0.18
16e graphic file with name nihms877330t5.jpg 34 [96±5] 7.48±0.09
16f graphic file with name nihms877330t6.jpg 78 [80±11] 7.13±0.11
16g graphic file with name nihms877330t7.jpg 41 [89±11] 7.41±0.11
16h graphic file with name nihms877330t8.jpg 38 [83±10] 7.48±0.17
16i graphic file with name nihms877330t9.jpg 29 [82±5] 7.74±0.22
16j graphic file with name nihms877330t10.jpg 76 [75±6] 7.12±0.08
16k graphic file with name nihms877330t11.jpg Inactive Inactive
16l graphic file with name nihms877330t12.jpg 17 [88±11] 7.77±0.01
16m graphic file with name nihms877330t13.jpg 16 [90±7] 7.81±0.03
16n graphic file with name nihms877330t14.jpg 185 [87±4] 6.80±0.19
16o graphic file with name nihms877330t15.jpg 51 [86±6] 7.30±0.00
16p graphic file with name nihms877330t16.jpg 8 [86±3] 8.09±0.05
16q graphic file with name nihms877330t17.jpg 11 [84±5] 7.97±0.09
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.