Table 1.
Functional M1 selectivity in vitro of VU0357017, xanomeline, 77-LH-28-1, and BQCA
| EC50 [μM] | Ki [μM] | Reference | |||||
|---|---|---|---|---|---|---|---|
| M1 | M2 | M3 | M4 | M5 | D2 | ||
| VU0357017 | 0.198 | >30 | >30 | >30 | >30 | >10 | Lebois et al. 2009 |
| Xanomeline | 0.020 | 1 | 0.079 | 0.040 | 0.20 | nd | Langmead et al. 2008a |
| 0.0003 | 0.0925 | 0.005 | 0.052 | 0.042 | 0.264 | Heinrich et al. 2009 | |
| 77-LH-28-1 | 0.008 | >10 | 2.51 | >10 | >10 | nd | Langmead et al. 2008a |
| 0.002 | 0.765 | 0.159 | >10 | 0.206 | 0.06 | Heinrich et al. 2009 | |
| BQCA * | 0.845 | >100 | >100 | >100 | >100 | >37.5 | Ma et al. 2009 |
VU0357017 is an allosteric partial agonist, xanomeline and 77-LH-28-1 are orthosteric agonists, BQCA a positive allosteric modulator.
*
Because BQCA is a positive modulator, not an agonist, no EC50 values could be determined, and M1 value represents the inflexion point (potentiation of 3 nM acetylcholine).
nd: not determined