Table 3.
Structures and activities for M4 PAM analogs 17.
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---|---|---|---|
Cmpd | R | hM4 EC50 (nM)a [% ACh Max ±SEM] | hM4 pEC50 (±SEM) |
17a |
![]() |
25 [85±8] | 7.61±0.08 |
17b |
![]() |
28 [82±9] | 7.56±0.03 |
17c |
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282 [77±8] | 6.55±0.04 |
17d |
![]() |
141 [77±11] | 6.88±0.11 |
17e |
![]() |
1289 [81±8] | 5.90±0.06 |
17f |
![]() |
934 [86±1] | 6.03±0.04 |
17g |
![]() |
325 [75±13] | 6.63±0.29 |
17h |
![]() |
37 [94±9] | 7.49±0.12 |
17i |
![]() |
30 [84±5] | 7.54±0.06 |
17j |
![]() |
19 [88±5] | 7.73±0.06 |
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.