Table 4

Parameters for the interaction of CMB with [3H]NMS and ACh at m1—m5 muscarinic receptors

SubtypeAssayLog affinityCooperativityn
Unoccupied receptor[3H]NMS-occupied receptor[3H]NMSACh
m1Nonequilibrium4.44  ± 0.084.23  ± 0.110.63  ± 0.043
Equilibrium4.38  ± 4.104.10  ± 0.200.54  ± 0.070.45  ± 0.054
m2Nonequilibrium4.28  ± 0.034.41  ± 0.011.36  ± 0.092
Equilibrium4.22  ± 0.114.37  ± 0.121.38  ± 0.030.094  ± 0.0194
m3Nonequilibrium3.71  ± 0.033.42  ± 0.020.52  ± 0.013
Equilibrium3.66  ± 0.133.26  ± 0.230.43  ± 0.113.26  ± 0.234
m4Nonequilibrium4.29  ± 0.044.32  ± 0.051.08  ± 0.143
Equilibrium4.32  ± 0.034.32  ± 0.084-a 1.08  ± 0.091.03  ± 0.144
m5Nonequilibrium
Equilibrium3.66  ± 0.043.26  ± 0.040.40  ± 0.010.055  ± 0.0102
  • 4-a n = 2, log affinity at the [3H]NMS-occupied receptor was fixed at 4.37 in two assays.