U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Approval Year

Substance Class Protein
Created
by admin
on Tue Apr 01 18:29:43 GMT 2025
Edited
by admin
on Tue Apr 01 18:29:43 GMT 2025
Protein Sub Type
Sequence Type COMPLETE
Record UNII
1PE72K8X46
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MU-TYPE OPIOID RECEPTOR
Common Name English
HMOP
Preferred Name English
MU OPIOID RECEPTOR
Common Name English
M-OR-1
Common Name English
MOR1
Common Name English
MOP
Common Name English
hMOP
Common Name English
mu (MOP)
Common Name English
MOR-1
Common Name English
MU OPIATE RECEPTOR
Common Name English
Code System Code Type Description
UNIPROT
P35372
Created by admin on Tue Apr 01 18:29:43 GMT 2025 , Edited by admin on Tue Apr 01 18:29:43 GMT 2025
PRIMARY
FDA UNII
1PE72K8X46
Created by admin on Tue Apr 01 18:29:43 GMT 2025 , Edited by admin on Tue Apr 01 18:29:43 GMT 2025
PRIMARY
From To
1_142 1_219
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_9
N 1_12
N 1_33
N 1_40
N 1_48
Related Record Type Details
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Emax = 81% of Fentanyl
EC50
AGONIST -> TARGET
INHIBITOR -> TARGET
PARTIAL AGONIST->TARGET
[35S]GTP?S Binding, 28.7 +/- 1.1 simulation
EC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
WEAK AGONIST->TARGET
Inhibition of forskolin-induced cAMP accumulation
IC50
INHIBITOR -> TARGET
AGONIST -> TARGET
INVERSE AGONIST->TARGET
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Reported to have 13X the potency of morphine
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed activity
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
An opioid analgesic drug from the thiambutene family, which has around the same potency as morphine.
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
INHIBITOR -> TARGET
In contrast to naloxone, diprenorphine (0.03 mgkg?1i.p.)reversed equipotent doses of morphine and fentanyl to the same degree. Assay done on SH-SY5Y cells displacing [3H]DIPRENORPHINE.
Ki
AGONIST -> TARGET
Assumed from being on CDC list
LIGAND->TARGET
BINDING
IC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
RADIOLIGAND->TARGET
Kd
AGONIST -> TARGET
AGONIST -> TARGET
Mini Gi assay. Emax=129 (123-136) relative to Fentanyl. EC50 for Fentanyl=34.6
EC50
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
Ki
AGONIST -> TARGET
Ki
AGONIST -> TARGET
Male, Wistar rats
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
EC50
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
EC50
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
Assumed activity
AGONIST -> TARGET
IC50
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Inhibition of cAMP accumulation
AGONIST -> TARGET
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 2.5
AGONIST
IC50
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
Blood furanylfentanyl concentrations are expected to be in a range of 1-45 ?g/L in victims of fatal overdosage.[
AGONIST -> TARGET
Assumed an agonist
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
PARTIAL AGONIST->TARGET
Emax = 23% of DAMGO
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
HUMAN RECEPTOR
AGONIST
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
EC50
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Potency higher than fentanyl (IC50=1.23 NM) fast onset and short duration of action.
IC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
INHIBITOR -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Emax=90% Relative maximum effect induced by stimulation with DAMGO. MOR functionality (EC50) measuring cyclic AMP (cAMP) on CHO-K1 cells.
EC50
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
BINDING
Ki
WEAK AGONIST->TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Ki
AGONIST -> TARGET
AGONIST -> TARGET
(+)-isomer
COMPETITIVE INHIBITOR
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
Cannot cross blood-brain barrier due to positive charge
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
Ki
LIGAND->BINDER
IC50
AGONIST -> TARGET
AGONIST -> TARGET
Ki
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
Mouse hot plate test. 117 times more potent than morphine.
ED50
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
In mouse hot plate test, the antinociceptive ED50 of C8813 was 11.5 ?g/kg, being 591 times and 3.4 times more potent than morphine and fentanyl respectively.
Ki
AGONIST -> TARGET
RADIOLIGAND->TARGET
Kd
AGONIST -> TARGET
Assumed active
INHIBITOR -> TARGET
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Herkinorin is a ?-opioid agonist with more than 100x higher ?-opioid affinity and 50x lower ?-opioid affinity compared to Salvinorin A.
AGONIST -> TARGET
Ratio to morphine 2.3
EC50
INHIBITOR -> TARGET
Mu Receptor [3H]DAMGO BINDING INHIBITION
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
PARTIAL AGONIST->TARGET
MOR partial agonists with reduced ?-arrestin-2 recruitment in-vitro. 20-fold more potent than morphine at inhibiting contractions and 100-fold more potent than mitragynine.
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
EC50
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
3H-DAMGO specific binding to gerbil ccrebellar membranes.
Ki
AGONIST -> TARGET
Opioid activity is due to both low affinity binding of the parent compound and higher affinity binding of the O-demethylated metabolite M1 to ?-opioid receptors. In animal models, M1 is up to 6 times more potent than tramadol in producing analgesia and 200 times more potent in ?-opioid binding.
AGONIST -> TARGET
Assumed from being on CDC list
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
The fluorinated MT?45 derivatives have higher apparent potencies (2F?MT?45: 42 nM) than MT?45 (1.3 ?M) for inhibition of cAMP accumulation and ??arrestin2 recruitment (2F?MT?45: 196 nM; MT?45: 23.1 ?M).
EC50
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Emax=94.9 relative to Fentanyl
EC50
AGONIST -> TARGET
Assumed from being on CDC list
INHIBITOR -> TARGET
AGONIST -> TARGET
Has around 7.5-fold the potency of morphine in animal models.
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Atypical. G-protein activation
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
INHIBITOR -> TARGET
ANTAGONIST
AGONIST -> TARGET
EC50
AGONIST -> TARGET
Assumed from being on CDC list
INHIBITOR -> TARGET
AGONIST -> TARGET
EC50
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
ED50(mg/kg) = 0.220, Potency ratio to morphine = 1.5, Potency ratio to fentanyl = 0.03
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
INHIBITOR -> TARGET
IC50
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
RADIOLIGAND->OFF TARGET
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
The antinociceptive ED50 in mouse hot plate of the two compounds were 11.5 ?g/kg and 13.4 ?g/kg respectively.
Ki
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Lance Ultra cAMP Assay
EC50
AGONIST -> TARGET
Lance Ultra cAMP Assay
EC50
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Lance Ultra cAMP Assay
EC50
AGONIST -> TARGET
In vitro data suggest that flunitazene is much less potent than fentanyl. Emax=118% of Fentanyl
EC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Emax=134% of Fentanyl
EC50
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
TRV0109662 is a weak (EC50= 5 mcM) partial agonist of the human mu-opioid receptor.
PARTIAL AGONIST
EC50
INHIBITOR->OFF-TARGET
Ki
AGONIST -> TARGET
WEAK AGONIST->TARGET
POTENCY
AGONIST -> TARGET
Assumed from being on CDC list
NON-INHIBITOR->OFF TARGET
ED50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
Emax=106 of Fentanyl
EC50
AGONIST -> TARGET
Ki
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
AGONIST -> TARGET
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 4.0
AGONIST
IC50
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
INHIBITOR -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Emax =140% of Fentanyl. In vitro data shows that N-desethyl isotonitazene is similar in potency to etonitazene, and approximately 20 times more potent than fentanyl.
EC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
Inhibition of forskolin-induced cAMP accumulation.
IC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Rat tail withdrawal test. Morphine ED50 3.15. Fentanyl ED50 0.1 mg/mL
ED50
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
Assumed active
INHIBITOR -> TARGET
AGONIST -> TARGET
An active opioid with potency approximately two times greater than that of fentanyl [unpublished data from L. De Vrieze and C. Stove].
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
An active opioid with potency approximately 25 times greater than that of fentanyl [unpublished data from L. De Vrieze and C. Stove].
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
EC50
AGONIST -> TARGET
Very high affinity for receptor
IC50
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
Butonitazene is tens of times superior to morphine when administered intravenously, as was found in chemical studies in rodents. Emax=103% of Fentanyl. beta-Arrestin assay
EC50
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Mouse hot plate test. 1516 times more potent than morphine.
ED50
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
AGONIST -> TARGET
WEAK AGONIST->TARGET
Presumed to be weak agonist.
AGONIST -> TARGET
10 times more potent than Fentanyl.
AGONIST -> TARGET
Emax 180 of hydromorphone
BIOASSAY (CELLULAR)
EC50
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
AGONIST -> TARGET
Ki
AGONIST -> TARGET
POTENCY
INHIBITOR -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 2.1
AGONIST
IC50
AGONIST -> TARGET
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
Prolonged exposure methadone induces MOPr internalization comparable with that induced by DAMGO, whereas morphine produces much less MOPr heroin during relapse is due to receptor internalization. The blunting of the response to desensitization not receptor antagonism.
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
AGONIST -> TARGET
Assumed from being on CDC list
AGONIST -> TARGET
EC50
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
Emax=113% relative to Fentanyl
EC50
AGONIST -> TARGET
Mouse hot plate test. 2600 times more potent than morphine.
ED50
AGONIST -> TARGET

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO ACID SUBSTITUTION [1_365] [1_377] DEXFOSFOSERINE VI4F0K069V
AMINO ACID SUBSTITUTION [1_372] THREONINE PHOSPHATE 3L4WX7B1EI
AMINO ACID SUBSTITUTION [1_168] TYROSINE O-PHOSPHATE 2R86C98KDX
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT CHEMICAL