. 2017 Oct 16;2(10):6741–6754. doi: 10.1021/acsomega.7b01085

Table 3. M₂R Binding Data (pK_i or pIC₅₀ Values) of Various Orthosteric (1 and 6), Allosteric (13–15), Dualsteric (7 and 10) MR Ligands, and 64 Determined with [³H]44, [³H]64, or [³H]5.

ligand	[³H]44 pK_i^a	[³H]64 pK_i^a	[³H]5 pK_i* or pIC₅₀**^b
1		5.78 ± 0.05	6.55 ± 0.05*
6	8.52 ± 0.26	8.52 ± 0.14	9.04 ± 0.08*
7		7.71 ± 0.14	8.71 ± 0.05*
10	9.61 ± 0.11	8.35 ± 0.09	9.11 ± 0.05*
13		5.60 ± 0.07	6.11 ± 0.09**^c
14	5.90 ± 0.22	6.08 ± 0.28	6.32 ± 0.18**^c
15		5.43 ± 0.02	<4.5**^c
64		9.44 ± 0.01	9.44 ± 0.06*

Determined by equilibrium competition binding with [³H]44 (2 nM) or [³H]64 (0.3 nM) at CHO-hM₂R cell homogenates; mean values ± SEM from at least three independent experiments (performed in triplicate).

Determined by equilibrium competition binding with [³H]5 (0.2 nM) at live CHO-hM₂R cells; mean ± SEM from at least three independent experiments (performed in triplicate).

Reported by Pegoli et al.²³

Table 3. M2R Binding Data (pKi or pIC50 Values) of Various Orthosteric (1 and 6), Allosteric (13–15), Dualsteric (7 and 10) MR Ligands, and 64 Determined with [3H]44, [3H]64, or [3H]5.

Table 3. M₂R Binding Data (pK_i or pIC₅₀ Values) of Various Orthosteric (1 and 6), Allosteric (13–15), Dualsteric (7 and 10) MR Ligands, and 64 Determined with [³H]44, [³H]64, or [³H]5.