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Table 1 Binding affinities for hMOR and Ala348,353 hMOR stably expressed in HEK 293 cells. Competition experiments were as described in the Experimental Procedures. Data are given as the mean ± S.E.M. from at least 3 independent experiments performed in triplicate. Statistical analysis was performed using Student's t test: the asterisks (*p < 0.05) refer to Ki values significantly different from corresponding Ki values for hMOR.

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

Ligand

hMOR

Ala348,353 hMOR

 
 

Ki(nM)

Ki(nM)

KiAla 348,353hMOR/KihMOR

Diprenorphine (Kd)

0.21 ± 0.03

0.41 ± 0.04

 

DAMGO

3.60 ± 0.44

1.13 ± 0.53*

0.32

Dermorphin

4.10 ± 1.70

0.26 ± 0.10*

0.06

Morphine

18.87 ± 4.76

0.88 ± 0.06*

0.05

β-endorphin

1.35 ± 0.42

2.45 ± 1.01

1.81

Dynorphin A

4.12 ± 0.85

1.59 ± 0.86

0.39

Met-enkephalin

2.78 ± 0.12

2.53 ± 0.58

0.91

Endomorphin 1

8.73 ± 2.66

0.51 ± 0.17*

0.06

Endomorphin 2

11.70 ± 3.90

1.79 ± 0.83*

0.15

Naloxone

3.63 ± 1.45

0.99 ± 0.25

0.27

Naltrexone

0.55 ± 0.22

0.17 ± 0.01

0.31

Naltrindole

5.07 ± 0.58

5.42 ± 0.56

1.06

Naloxonazine

2.91 ± 0.97

1.06 ± 0.23

0.36

Nalbuphine

2.28 ± 0.79

0.66 ± 0.05

0.29

CTOP

5.46 ± 0.70

0.32 ± 0.05*

0.06

Cyprodime

23.12 ± 7.22

1.83 ± 0.40*

0.08