Table 1 Pharmacological parameters from fitting agonist curves to the three different models presented in Fig. 6 as estimated by nonlinear regression for each equation

From: Characterization of the GTPγS release function of a G protein-coupled receptor

 

Stephenson’s Efficacy

Two-State Efficacy

Operational Efficacy

 

Emax εBinding

Emax εRelease

LogEC50 Binding

LogEC50 Release

Two-state αBinding

Two-state αRelease

Two-state logKBinding

Two-state logKRelease

Operational τBinding

Operational τRelease

Operational logKBinding

Operational logKRelease

DAMGO

1

1

-8.0 ± 0.04

-7.8 ± 0.05

nd

nd

nd

nd

nd

nd

nd

nd

Morphine

1.02 ± 0.03a

0.84 ± 0.01a

-7.5 ± 0.06

-7.5 ± 0.08

nde

511.2 ± 103.9e

nd

-6.7 ± 0.13

ndh

6.73 ± 0.13 h

nd

-6.7 ± 0.13

Fentanyl

1.02 ± 0.03b

0.92 ± 0.01b

-7.6 ± 0.04

-7.7 ± 0.16

ndf

1061 ± 449.1 f

nd

-6.6 ± 0.22

ndi

6.56 ± 0.21i

nd

-6.6 ± 0.21

Buprenorphine

0.47 ± 0.02

0.51 ± 0.02

-8.9 ± 0.02 d

-10.1 ± 0.06 d

100.6 ± 4.3

100.6 ± 4.3

-8.5 ± 0.07

-9.8 ± 0.07

1.04 ± 0.05

1.04 ± 0.05

-8.5 ± 0.1

-9.8 ± 0.1

Nalbuphine

0.17 ± 0.02c

0.35 ± 0.05c

-8.0 ± 0.11

-8.3 ± 0.13

20.5 ± 1.02 g

54.9 ± 5.6 g

-7.8 ± 0.09

-8.1 ± 0.17

0.20 ± 0.01j

0.54 ± 0.05j

-7.9 ± 0.55

-8.1 ± 0.14

  1. Each parameter estimate is the product of 3-6 experiments.
  2. aStudent’s unpaired two-tail t-test p = 0.0065.
  3. bStudent’s unpaired two-tail t-test p = 0.0398.
  4. cStudent’s unpaired two-tail t-test p = 0.0214.
  5. dStudent’s unpaired two-tail t-test p < 0.0001.
  6. eextra sum-of-squares F test: 19.95 (1, 44), p < 0.001.
  7. fextra sum-of-squares F test: 6.617 (1, 44), p = 0.0136.
  8. gextra sum-of-squares F test: 25.68 (1, 44), p < 0.001.
  9. hextra sum-of-squares F test: 24.46 (1, 26), p < 0.001.
  10. iextra sum-of-squares F test: 6.994 (1, 26), p = 0.0137.
  11. jextra sum-of-squares F test: 26.12 (1, 26), p < 0.001.
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