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Table 3 Binding parameters of NMS, ACh and rapacuronium to membranes from CHO cells expressing M1 through M5 receptor subtypes.

From: Divergence of allosteric effects of rapacuronium on binding and function of muscarinic receptors

 

[3H]NMS

[3H]Ach

Ach

   

high affinity binding

low affinity binding

 

pKA

pKA

pKA

M1

5.37 ± 0.03

-1.08 ± 0.05

5.37 ± 0.04

-1.30 ± 0.07

5.33 ± 0.03

-1.32 ± 0.06

M2

5.59 ± 0.03

-0.83 ± 0.07

5.55 ± 0.05

-1.46 ± 0.08

5.56 ± 0.04

-1.52 ± 0.06

M3

4.75 ± 0.04

-1.11 ± 0.05

4.80 ± 0.04

-1.26 ± 0.05

4.77 ± 0.05

-1.20 ± 0.07

M4

5.42 ± 0.04

-1.40 ± 0.04

5.41 ± 0.05

-1.51 ± 0.05

5.49 ± 0.04

-1.56 ± 0.07

M5

4.97 ± 0.04

-1.54 ± 0.05

4.92 ± 0.03

-1.34 ± 0.07

4.95 ± 0.04

-1.28 ± 0.07

  1. Negative logarithm of equilibrium dissociation constant of rapacuronium (pKA) and factor of cooperativity (α ) between rapacuronium and radioligand ([3H]NMS or [3H]ACh, respectively) binding were obtained by fitting Eq. 3 to the data in Figures 4 and 5. Negative logarithm of equilibrium dissociation constant of rapacuronium (pKA) and factors of cooperativity (β) between rapacuronium and acetylcholine low affinity binding were obtained by fitting Eq. 4 to the data in Figure 5. Factors of cooperativity α and β are expressed as negative logarithms so that negative values represent negative cooperativity. Values are means ± SE of fits to 3 independent experiments performed in quadruplicates.