U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Substance Class Protein
Created
by admin
on Sat Dec 16 12:09:21 UTC 2023
Edited
by admin
on Sat Dec 16 12:09:21 UTC 2023
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
MU OPIOID RECEPTOR
Common Name English
M-OR-1
Common Name English
MOR1
Common Name English
MOP
Common Name English
hMOP
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 Sat Dec 16 12:09:33 UTC 2023 , Edited by admin on Sat Dec 16 12:09:33 UTC 2023
PRIMARY
FDA UNII
1PE72K8X46
Created by admin on Sat Dec 16 12:09:33 UTC 2023 , Edited by admin on Sat Dec 16 12:09:33 UTC 2023
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
Emax = 81% of Fentanyl
EC50
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
WEAK AGONIST->TARGET
Inhibition of forskolin-induced cAMP accumulation
IC50
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Reported to have 13X the potency of morphine
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
An opioid analgesic drug from the thiambutene family, which has around the same potency as morphine.
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
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
LIGAND->TARGET
BINDING
IC50
AGONIST -> TARGET
AGONIST -> TARGET
ANTAGONIST->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
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
Ki
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
EC50
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
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
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
Blood furanylfentanyl concentrations are expected to be in a range of 1-45 μg/L in victims of fatal overdosage.[
AGONIST -> TARGET
Assumed an agonist
PARTIAL AGONIST->TARGET
Emax = 23% of DAMGO
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
HUMAN RECEPTOR
AGONIST
Ki
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
EC50
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
Potency higher than fentanyl (IC50=1.23 NM) fast onset and short duration of action.
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Ki
AGONIST -> TARGET
AGONIST -> TARGET
(+)-isomer
COMPETITIVE INHIBITOR
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
Cannot cross blood-brain barrier due to positive charge
AGONIST -> TARGET
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 μg/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
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A.
INHIBITOR -> TARGET
Mu Receptor [3H]DAMGO BINDING INHIBITION
BINDING
Ki
PARTIAL AGONIST->TARGET
MOR partial agonists with reduced β-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
BINDING
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 μ-opioid receptors. In animal models, M1 is up to 6 times more potent than tramadol in producing analgesia and 200 times more potent in μ-opioid binding.
PARTIAL AGONIST->TARGET
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 μM) for inhibition of cAMP accumulation and β‐arrestin2 recruitment (2F‐MT‐45: 196 nM; MT‐45: 23.1 μM).
EC50
WEAK AGONIST->TARGET
Emax=91.2% of Fentanyl
EC50
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
Emax=94.9 relative to Fentanyl
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
Has around 7.5-fold the potency of morphine in animal models.
AGONIST -> TARGET
Atypical. G-protein activation
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
ANTAGONIST
AGONIST -> TARGET
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
EC50
AGONIST -> TARGET
EC50
AGONIST -> TARGET
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
RADIOLIGAND->OFF TARGET
Ki
AGONIST -> TARGET
The antinociceptive ED50 in mouse hot plate of the two compounds were 11.5 μg/kg and 13.4 μg/kg respectively.
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Lance Ultra cAMP Assay
EC50
AGONIST -> TARGET
Lance Ultra cAMP Assay
EC50
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
AGONIST -> TARGET
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
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
NON-INHIBITOR->OFF TARGET
ED50
AGONIST -> TARGET
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
POTENCY
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Inhibition of forskolin-induced cAMP accumulation.
IC50
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
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
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
PARTIAL AGONIST
BINDING
Ki
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
AGONIST -> TARGET
EC50
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
Mouse hot plate test. 1516 times more potent than morphine.
ED50
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
AGONIST -> TARGET
POTENCY
INHIBITOR -> TARGET
AGONIST -> TARGET
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 2.1
AGONIST
IC50
AGONIST -> TARGET
AGONIST -> TARGET
EC50
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
POTENCY
INHIBITOR -> TARGET
AGONIST -> TARGET
BINDING
Ki
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
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
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT CHEMICAL