. 2020 Jun 8;11(7):823–832. doi: 10.1039/d0md00137f

Table 1. M₁–M₅ receptor binding data (pK_i values) of compounds 7 and 15–20 obtained from radioligand competition binding studies, and M₂R binding data (pK_d values) from flow cytometric saturation binding experiments.

Compd.	pK_i ^a					pK_d ^b
Compd.	M₁R	M₂R	M₃R	M₄R	M₅R	M₂R
7 (ref. 47)	7.86	8.52	6.83	8.02	6.41	8.63 ± 0.08
15 (UR-CG072)	8.21 ± 0.02	8.75 ± 0.07	6.89 ± 0.06	8.43 ± 0.07	6.56 ± 0.10	8.36 ± 0.09
16 (UR-CG073)	9.00 ± 0.13	9.16 ± 0.10	7.43 ± 0.13	9.38 ± 0.05	8.00 ± 0.08	8.41 ± 0.10
17 (UR-CG074)	8.15 ± 0.05	8.87 ± 0.08	7.16 ± 0.01	8.58 ± 0.08	7.39 ± 0.07	8.70 ± 0.04
18 (UR-AP175)	8.31 ± 0.04	9.04 ± 0.15	7.07 ± 0.04	8.37 ± 0.04	7.15 ± 0.06	8.74 ± 0.13
19 (UR-CG135)	8.32 ± 0.03	9.02 ± 0.10	7.20 ± 0.15	8.57 ± 0.01	6.90 ± 0.03	9.19 ± 0.03
20 (UR-MK342)	8.59 ± 0.10	9.62 ± 0.04	7.09 ± 0.06	9.01 ± 0.03	6.75 ± 0.05	8.86 ± 0.06

^aDetermined by competition binding with [³H]NMS (K_d values/applied concentrations: M₁, 0.17/0.2 nM; M₂, 0.10/0.2 nM; M₃, 0.12/ 0.2 nM; M₄, 0.052/0.1 nM; M₅, 0.20/0.3 nM) at whole CHO–hM_xR cells (x = 1-5) at 23 °C. Means ± SEM from two (20, M₅R) or at least three independent experiments (each performed in triplicate).

^bDetermined by flow cytometric saturation binding experiments at intact CHO–hM₂R cells at 22 °C. Means ± SEM from two (20) or at least three independent experiments (performed in duplicate).

Table 1. M1–M5 receptor binding data (pKi values) of compounds 7 and 15–20 obtained from radioligand competition binding studies, and M2R binding data (pKd values) from flow cytometric saturation binding experiments.

Table 1. M₁–M₅ receptor binding data (pK_i values) of compounds 7 and 15–20 obtained from radioligand competition binding studies, and M₂R binding data (pK_d values) from flow cytometric saturation binding experiments.