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Table 5 Effects of rapacuronium on ACh-stimulated [35S]GTPγS binding

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

 

Acetylcholine

+ 0.1 μM rapacuronium

+ 1 μM rapacuronium

+ 10 μM rapacuronium

 

pEC50

EMAX

pEC50

EMAX

pEC50

EMAX

pEC50

EMAX

M1

5.20 ± 0.05

2.23 ± 0.08

5.41 ± 0.04*

2.35 ± 0.12

5.78 ± 0.04*

2.28 ± 0.12

5.22 ± 0.05

2.27 ± 0.11

M2

6.61 ± 0.03

3.12 ± 0.12

6.65 ± 0.03

3.10 ± 0.15

5.92 ± 0.05*

2.93 ± 0.13

5.67 ± 0.07*

2.46 ± 0.18*

M3

5.31 ± 0.05

2.12 ± 0.08

5.65 ± 0.04*

2.78 ± 0.11*

5.66 ± 0.04*

2.52 ± 0.08*

4.83 ± 0.05*

2.12 ± 0.09

M4

5.95 ± 0.04

2.93 ± 0.15

5.93 ± 0.04

2.95 ± 0.11

5.59 ± 0.05*

2.80 ± 0.12

5.12 ± 0.05*

2.32 ± 0.16*

M5

5.26 ± 0.05

1.99 ± 0.08

5.45 ± 0.04*

2.10 ± 0.09

5.82 ± 0.04*

2.04 ± 0.09

5.29 ± 0.05

2.22 ± 0.09

  1. Negative logarithms of half effective concentrations (pEC50) and maximum stimulatory effect (EMAX) of acetylcholine on [35S]GTPγS binding in the absence or presence of the indicated concentrations of rapacuronium were obtained by fitting Eq. 5 to the data in Figure 6. Values are means ± SE of fits to 3 independent experiments performed in quadruplicates. *P < 0.05; significantly different from control (Ach alone) by ANOVA and Tukey-Kramer post-test.