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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