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Table 2 Classification of opioid ligands based on their DMR agonist activity in the five distinct cell lines

From: Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family

Name HEK MOR DOR KOR SH-SY5Y Literature classification
β-Funaltrexamine off-target Partial agonist Partial agonist Partial agonist   Mu antagonist
BNTX off-target off-target off-target off-target off-target Delta antagonist
Dynorphin A (2–13) off-target   Partial agonist Partial agonist   Kappa agonist
Etonitazenyl off-target Partial agonist   Partial agonist   Mu agonist
ICI 199,441 off-target Full agonist Partial agonist Full agonist   Kappa agonist
Nociceptin (1–13) off-target Partial agonist   Partial agonist   ORL1 agonist
α-Neoendorphin   Partial agonist Full agonist Full agonist Full agonist Kappa agonist
BRL-52537    Partial agonist Full agonist   Kappa agonist
BUBUC   Partial agonist Full agonist Partial agonist Partial agonist Delta agonist
DADLE   Partial agonist Full agonist Partial agonist Full agonist Delta agonist
DALDA   Partial agonist    Full agonist Mu agonist
DAMGO   Full agonist Partial agonist Partial agonist Full agonist Mu agonist
DAMME   Full agonist Full agonist Partial agonist Full agonist Mu/Delta agonist
Deltorphin II   Partial agonist Full agonist    Delta agonist
DIPPA   Partial agonist Partial agonist Full agonist   Kappa antagonist
DPDPE   Partial agonist Full agonist Partial agonist Full agonist Delta agonist
DSLET   Full agonist Full agonist Partial agonist Full agonist Delta agonist
DTLET   Full agonist Full agonist Partial agonist Full agonist Delta agonist
Dynorphin A (1–13)   Full agonist Full agonist Full agonist Partial agonist Kappa agonist
Dynorphin A (1–8)   Full agonist Full agonist Full agonist Full agonist Kappa agonist
Dynorphin B   Partial agonist Full agonist Full agonist Full agonist Kappa agonist
Endomorphin-1   Partial agonist Partial agonist   Partial agonist Mu agonist
Endomorphin-2   Partial agonist Partial agonist Partial agonist Full agonist Mu agonist
(Leu5)-Enkephalin   Full agonist Full agonist Partial agonist Full agonist Mu/Delta agonist
(Met5)-Enkephalin   Full agonist Full agonist Partial agonist Full agonist Mu/Delta agonist
GR 89696   Partial agonist Partial agonist Full agonist Full agonist Kappa agonist
ICI 204,448   Partial agonist Partial agonist Full agonist Full agonist Kappa agonist
Levallorphan    Partial agonist Partial agonist   Partial Mu/delta agonist
Morphiceptin   Partial agonist    Partial agonist Mu agonist
Nalbuphine   Partial agonist Partial agonist Partial agonist   Partial Mu/kappa agonist
Naloxonazine     Partial agonist   Mu antagonist
Naloxone HCl       Opioid antagonist
Naloxone methiodide       Opioid antagonist
Naltrexone     Partial agonist   Opioid antagonist
Naltriben       Delta antagonist
Naltrindole       Delta antagonist
N-Benzylnaltrindole    Partial agonist Partial agonist   Delta antagonist
N-MPPP   Partial agonist Partial agonist Full agonist   Kappa agonist
NNC 63-0532   Partial agonist Partial agonist Partial agonist Full agonist ORL1 agonist
Nociceptin     Partial agonist   ORL1 agonist
Nor-Binaltorphimine       Kappa antagonist
(−)-Norcodeine   Partial agonist   Partial agonist Partial agonist Opioid antagonist
Salvinorin A   Partial agonist   Full agonist   Kappa agonist
SKF10047    Partial agonist Partial agonist   Opioid agonist/antagonist
SNC 121    Partial agonist Partial agonist Partial agonist Delta agonist
SNC 80   Partial agonist Partial agonist Partial agonist Partial agonist Delta agonist
Syndyphalin SD-25   Full agonist Partial agonist Partial agonist Partial agonist Mu agonist
TAPP   Partial agonist Partial agonist Partial agonist Full agonist Mu agonist
Tramadol   Partial agonist     Weak Mu agonist
(−)-U-50488   Partial agonist Partial agonist Full agonist   Kappa partial agonist
(+)-U-50488     Full agonist   Kappa partial agonist
U-50,488H   Partial agonist Partial agonist Full agonist   Kappa agonist
U-54494A   Partial agonist Partial agonist Partial agonist   Kappa agonist
U-62066   Partial agonist   Full agonist   Kappa agonist
U-69593   Partial agonist Partial agonist Full agonist   Kappa agonist
  1. The blank indicates that the ligand did not result in any noticeable DMR.