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Table 1 Effects of rapacuronium on [3H]NMS and [3H]ACh saturation binding

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

 

pKD

BMAX

pKD'

BMAX

pKD'

BMAX

 

[3H]NMS

+ 10 μM rapacuronium

+ 100 μM rapacuronium

M1

9.60 ± 0.04

1.98 ± 0.20

9.14 ± 0.03*

2.03 ± 0.15

8.73 ± 0.03*

1.85 ± 0.17

M2

9.49 ± 0.03

1.56 ± 0.16

8.92 ± 0.04*

1.62 ± 0.14

8.64 ± 0.03*

1.66 ± 0.14

M3

9.64 ± 0.05

1.64 ± 0.17

9.44 ± 0.03*

1.67 ± 0.14

8.96 ± 0.03*

1.59 ± 0.16

M4

9.69 ± 0.04

1.19 ± 0.14

9.19 ± 0.02*

1.17 ± 0.13

8.52 ± 0.06*

1.06 ± 0.10

M5

9.59 ± 0.03

1.49 ± 0.16

9.31 ± 0.02*

1.53 ± 0.15

8.46 ± 0.06*

1.33 ± 0.13

 

[ 3 H]Ach

+ 10 μM rapacuronium

+ 100 μM rapacuronium

M1

7.58 ± 0.05

0.33 ± 0.05

7.12 ± 0.03*

0.33 ± 0.05

6.43 ± 0.05*

0.32 ± 0.05

M2

7.63 ± 0.03

0.80 ± 0.08

7.09 ± 0.05*

0.74 ± 0.07

6.30 ± 0.06*

0.77 ± 0.08

M3

7.67 ± 0.05

0.39 ± 0.05

7.43 ± 0.04*

0.40 ± 0.04

6.85 ± 0.03*

0.37 ± 0.05

M4

7.69 ± 0.04

0.55 ± 0.04

7.17 ± 0.03*

0.54 ± 0.05

6.41 ± 0.05*

0.47 ± 0.04

M5

7.68 ± 0.03

0.33 ± 0.06

7.43 ± 0.02*

0.33 ± 0.03

6.64 ± 0.04*

0.34 ± 0.06

  1. Negative logarithms of equilibrium dissociation constants (pKD) and maximum binding capacities (BMAX in fmol/μg of protein) of radioligands were obtained from saturation experiments shown in Figure 1 by fitting Eq. 1 to the data. Values are means ± SE of fits to 3 independent experiments performed in quadruplicates.
  2. *P < 0.05; significantly different from control (radioligand alone) by ANOVA and Tukey-Kramer post-test.