Table 2.
Functional Activity of TBPB Amide Analogues 14.
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|---|---|---|---|---|
| Cmpd | X | M1 EC50 (μM)a | %CCh Maxa | D2 IC50 (μM)a |
| 14a | 4-F | 2.6 | 49 | >10 |
| 14b | 5-F | 2.3 | 82 | 3.6 |
| 14c | 6-F | 3.3 | 76 | >10 |
| 14d | 5-Cl | 4.1 | 82 | 2.3 |
| 14e | 5-Br | 4.4 | 81 | 2.7 |
EC50s, % CCh maximum (measures M1 activation relative to 100% CCh response) and IC50s are the mean of at least three independent determinations. All analogues in this Table are selective for M1 (>30 M vs. M2–M5).
