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Table 2 Efficacy and potency of opioid agonists for the stimulation of [35S] GTPγS binding in HEK 293 cells stably expressing hMOR or Ala348,353 hMOR. Agonist efficacy was calculated as the maximal difference between specific [35S] GTPγS binding in the presence and absence of agonist and is expressed in fmol/mg. EC50 values were obtained from curve fitting of dose response curves shown in Figure 3. Receptor densities were 4.13 ± 0.26 and 1.5 ± 0.20 pmol/mg membrane protein for hMOR and Ala348,353 hMOR, respectively. Statistical analysis was performed using Student's t test: the asterisks (**p < 0.01, ***p < 0,001) refer to values significantly different from corresponding values for hMOR (Student's t test,)

From: Enhanced spontaneous activity of the mu opioid receptor by cysteine mutations: characterization of a tool for inverse agonist screening.

 

Basal

DAMGO

Morphine

  

Efficacy

EC50

Efficacy

EC50

 

fmol/mg

fmol/mg

nM

fmol/mg

nM

hMOR

25 ± 2

98 ± 10

81 ± 2

48 ± 7

176 ± 2

 

(n = 32)

(n = 10)

(n = 5)

(n = 3)

(n = 3)

Ala348,353 hMOR

41 ± 2.5***

58 ± 6 ***

9.1 ± 2.4**

48 ± 5

60 ± 2**

 

(n = 18)

(n = 9)

(n = 4)

(n = 4)

(n = 4)