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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 1.

Structures and activities for M4 PAM analogs 6.

graphic file with name nihms877330u2.jpg
Cmpd R hM4 EC50 (nM)a [% ACh Max ±SEM] hM4 pEC50 (±SEM)
6a CO2Bn 30 [81±8] 7.62±0.19
6b CO2Ph 23 [96±3] 7.65±0.03
6c CO2(3-Me)Ph 67 [85±9] 7.23±0.17
6d C(O)NHPh 217 [89±6] 6.66±0.03
6e SO2Ph 268 [70±8] 6.58±0.07
6f C(O)Ph 773 [85±6] 6.22±0.25
6g C(O)2-pyridyl 564 [91±5] 6.25±0.03
6h C(O)4-pyridyl 179 [85±7] 6.75±0.03
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.