Parameters for the interaction of CMB with [3H]NMS and ACh at m1—m5 muscarinic receptors
Subtype | Assay | Log affinity | Cooperativity | n | ||
---|---|---|---|---|---|---|
Unoccupied receptor | [3H]NMS-occupied receptor | [3H]NMS | ACh | |||
m1 | Nonequilibrium | 4.44 ± 0.08 | 4.23 ± 0.11 | 0.63 ± 0.04 | 3 | |
Equilibrium | 4.38 ± 4.10 | 4.10 ± 0.20 | 0.54 ± 0.07 | 0.45 ± 0.05 | 4 | |
m2 | Nonequilibrium | 4.28 ± 0.03 | 4.41 ± 0.01 | 1.36 ± 0.09 | 2 | |
Equilibrium | 4.22 ± 0.11 | 4.37 ± 0.12 | 1.38 ± 0.03 | 0.094 ± 0.019 | 4 | |
m3 | Nonequilibrium | 3.71 ± 0.03 | 3.42 ± 0.02 | 0.52 ± 0.01 | 3 | |
Equilibrium | 3.66 ± 0.13 | 3.26 ± 0.23 | 0.43 ± 0.11 | 3.26 ± 0.23 | 4 | |
m4 | Nonequilibrium | 4.29 ± 0.04 | 4.32 ± 0.05 | 1.08 ± 0.14 | 3 | |
Equilibrium | 4.32 ± 0.03 | 4.32 ± 0.084-a | 1.08 ± 0.09 | 1.03 ± 0.14 | 4 | |
m5 | Nonequilibrium | |||||
Equilibrium | 3.66 ± 0.04 | 3.26 ± 0.04 | 0.40 ± 0.01 | 0.055 ± 0.010 | 2 |
↵4-a n = 2, log affinity at the [3H]NMS-occupied receptor was fixed at 4.37 in two assays.