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

Morse, Megan; Sun, Haiyan; Tran, Elizabeth; Levenson, Robert; Fang, Ye

doi:10.1186/2050-6511-14-17

BMC Pharmacology and Toxicology

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

The blank indicates that the ligand did not result in any noticeable DMR.

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ISSN: 2050-6511

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