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

Approval Year

Unknown
134361
Substance Class Protein
Created
by admin
on Thu Jul 06 17:45:51 UTC 2023
Edited
by admin
on Thu Jul 06 17:45:51 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
MOR-1
Common Name English
MU OPIATE RECEPTOR
Common Name English
Code System Code Type Description
UNIPROT
P35372
Created by admin on Thu Jul 06 17:46:02 UTC 2023 , Edited by admin on Thu Jul 06 17:46:02 UTC 2023
PRIMARY
FDA UNII
1PE72K8X46
Created by admin on Thu Jul 06 17:46:02 UTC 2023 , Edited by admin on Thu Jul 06 17:46:02 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
Structure of ETODESNITAZENE PHENYLTHIOL ANALOGUE
AGONIST -> TARGET
POTENCY
Structure of THIAFENTANIL
AGONIST -> TARGET
Structure of METHYLNITAZENE
AGONIST -> TARGET
POTENCY
Structure of 4'-HYDROXYLNITAZENE
AGONIST -> TARGET
Emax = 81% of Fentanyl
EC50
Structure of N-PHENYLPROPYLNORFENTANYL
AGONIST -> TARGET
Structure of NALDEMEDINE 6-O-.BETA.-D-GLUCURONIDE
INHIBITOR -> TARGET
Structure of OLICERIDINE
AGONIST -> TARGET
Structure of TILIDINE
WEAK AGONIST->TARGET
Inhibition of forskolin-induced cAMP accumulation
IC50
Structure of BEVENOPRAN
INHIBITOR -> TARGET
PHENARIDINE
AGONIST -> TARGET
Structure of ISOBUTYRYLFENTANYL
AGONIST -> TARGET
Structure of CYCLOPROPYL FENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of 7-HYDROXYMITRAGYNINE
AGONIST -> TARGET
Reported to have 13X the potency of morphine
Ki
Structure of U-49900
AGONIST -> TARGET
Structure of PHENYLFENTANYL
AGONIST -> TARGET
Structure of AMDAKEFALIN
AGONIST -> TARGET
Structure of PYRIDIN-4-YLETHYL-NORFENTANYL
AGONIST -> TARGET
Structure of ETODESNITAZENE PYRROLIDINE ANALOGUE
AGONIST -> TARGET
POTENCY
Structure of PIPERIDYLTHIAMBUTENE
AGONIST -> TARGET
An opioid analgesic drug from the thiambutene family, which has around the same potency as morphine.
Structure of PSICOFENTANIL
AGONIST -> TARGET
Structure of ACRYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of ETONITAZEPIPNE
AGONIST -> TARGET
POTENCY
Structure of TETRAMETHYLCYCLOPROPYLFENTANYL
AGONIST -> TARGET
Structure of DIPRENORPHINE
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
Structure of BETA-METHYL ACETYL FENTANYL
AGONIST -> TARGET
Structure of THENYLFENTANYL
AGONIST -> TARGET
Structure of METHADONE
ANTAGONIST->TARGET
Structure of FAXELADOL
AGONIST -> TARGET
Structure of Protonitazene
AGONIST -> TARGET
Mini Gi assay. Emax=129 (123-136) relative to Fentanyl. EC50 for Fentanyl=34.6
EC50
Structure of ISOFENTANYL
AGONIST -> TARGET
Structure of 3-PHENYLPROPANOYLFENTANYL
AGONIST -> TARGET
Structure of BUTYRFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of MITRAGYNINE
AGONIST -> TARGET
Structure of MORPHINE
AGONIST -> TARGET
Ki
Structure of CYCLOBUTYLFENTANYL
AGONIST -> TARGET
EC50
Structure of METODESNITAZENE
WEAK AGONIST->TARGET
Emax=91.2% of Fentanyl
EC50
Structure of DIHYDROMORPHINE
AGONIST -> TARGET
Structure of ORTHO-FLUORO ACRYLFENTANYL
AGONIST -> TARGET
EC50
Structure of META-FLUOROFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of OCFENTANIL
AGONIST -> TARGET
Structure of DERMORPHIN
AGONIST -> TARGET
IC50
Structure of FURANYLETHYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of MT-45
AGONIST -> TARGET
Inhibition of cAMP accumulation
Structure of 2-CHLOROFENTANYL
AGONIST -> TARGET
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 2.5
AGONIST
IC50
Structure of PARAFLUOROISOBUTYRYLBENZYLFENTANYL
AGONIST -> TARGET
Structure of METHOXYACETYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of BETACETYLMETHADOL
AGONIST -> TARGET
Structure of BRORPHINE
AGONIST -> TARGET
Structure of METHYLTHIONITAZENE
AGONIST -> TARGET
POTENCY
Structure of 2,2'-DIFLUOROFENTANYL
AGONIST -> TARGET
Structure of 2-FURANYLFENTANYL
AGONIST -> TARGET
Blood furanylfentanyl concentrations are expected to be in a range of 1-45 μg/L in victims of fatal overdosage.[
Structure of N-Benzylfuranylfentanyl
AGONIST -> TARGET
Assumed an agonist
Structure of MP-135
PARTIAL AGONIST->TARGET
Emax = 23% of DAMGO
EC50
Structure of AXELOPRAN
INHIBITOR -> TARGET
Structure of BU-72
AGONIST -> TARGET
Structure of FENTANYL
AGONIST -> TARGET
HUMAN RECEPTOR
AGONIST
Ki
Structure of ORTHO-ISOPROPYLFURANYLFENTANYL
AGONIST -> TARGET
Structure of SAMERIDINE
PARTIAL AGONIST->TARGET
Structure of N-(MDA)-FENTANYL
AGONIST -> TARGET
Structure of ORTHO-METHOXYFURANYLFENTANYL
AGONIST -> TARGET
Structure of ORTHO-FLUOROBUTYRYL FENTANYL
AGONIST -> TARGET
EC50
Structure of BRONITAZENE
AGONIST -> TARGET
POTENCY
Structure of DIPYANONE
AGONIST -> TARGET
Structure of REMIFENTANIL
AGONIST -> TARGET
Potency higher than fentanyl (IC50=1.23 NM) fast onset and short duration of action.
IC50
Structure of PARA-METHOXYBUTYRYL FENTANYL
AGONIST -> TARGET
Structure of NALDEMEDINE
INHIBITOR -> TARGET
Structure of .ALPHA.-METHYL-.BETA.-HYDROXYFENTANYL
AGONIST -> TARGET
Structure of MIRFENTANIL
AGONIST -> TARGET
3-METHYLFENTANYL
AGONIST -> TARGET
NFEPP
AGONIST -> TARGET
Structure of BRIFENTANIL
AGONIST -> TARGET
Structure of ETHYLTHIONITAZENE
AGONIST -> TARGET
POTENCY
Structure of .BETA.-HYDROXYTHIOFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of ETODESNITAZENE PHENYLTHIOL/PYRROLIDINE ANALOGUE
AGONIST -> TARGET
POTENCY
Structure of BUPRENORPHINE
PARTIAL AGONIST->TARGET
PARTIAL AGONIST
BINDING
Ki
Structure of 4-FLUOROISOBUTYRFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of O-METHYL ACETYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of ACETYL-.ALPHA.-METHYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of IQMF-4
AGONIST -> TARGET
Ki
Structure of TEGILERIDINE
AGONIST -> TARGET
Structure of TRAMADOL
AGONIST -> TARGET
(+)-isomer
COMPETITIVE INHIBITOR
Ki
Structure of ALVIMOPAN
AGONIST -> TARGET
Structure of FRAKEFAMIDE
AGONIST -> TARGET
Structure of 4-FLUOROBUTYRFENTANYL
AGONIST -> TARGET
Structure of R-30490
AGONIST -> TARGET
Structure of CEBRANOPADOL
AGONIST -> TARGET
Structure of METHYLNALTREXONE
INHIBITOR -> TARGET
Cannot cross blood-brain barrier due to positive charge
Structure of 6-ACETYLMORPHINE
AGONIST -> TARGET
Structure of DIMETONITAZENE
AGONIST -> TARGET
POTENCY
Structure of ETODESNITAZENE PIPERIDINE ANALOGUE
AGONIST -> TARGET
POTENCY
Structure of 3-METHYLFENTANYL, (3S,4S)-
AGONIST -> TARGET
Mouse hot plate test. 117 times more potent than morphine.
ED50
Structure of PARA-CHLOROISOBUTYRYL FENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of THIOBROMADOL
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
Structure of 3-FURANYLFENTANYL
AGONIST -> TARGET
Structure of Diprenorphine H-3
RADIOLIGAND->TARGET
Kd
Structure of 4-HYDROXYBUTYRFENTANYL
AGONIST -> TARGET
Assumed active
Structure of ALVIMOPAN ANHYDROUS
INHIBITOR -> TARGET
Ki
Structure of TAPENTADOL
AGONIST -> TARGET
Structure of .ALPHA.-METHYL-BUTYRFENTANYL
AGONIST -> TARGET
Structure of METODESNITAZENE
AGONIST -> TARGET
POTENCY
Structure of ALFENTANIL
AGONIST -> TARGET
Structure of METHYL-AP-237
AGONIST -> TARGET
Structure of 3-METHYLTHIOFENTANYL
AGONIST -> TARGET
Structure of .BETA.-METHYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of HERKINORIN
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.
Structure of NALOXONE
INHIBITOR -> TARGET
Mu Receptor [3H]DAMGO BINDING INHIBITION
BINDING
Ki
Structure of MITRAGYNINE PSEUDOINDOXYL
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
Structure of NALTREXONE
INHIBITOR -> TARGET
Structure of 3-METHYLFENTANYL, TRANS-
AGONIST -> TARGET
EC50
Structure of NALTALIMIDE
PARTIAL AGONIST->TARGET
Structure of 4-METHYL CYCLOPROPYL FENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of DESMETRAMADOL
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.
Structure of .ALPHA.-METHYLFENTANYL
AGONIST -> TARGET
Structure of GPA-3154
PARTIAL AGONIST->TARGET
Structure of VALERYLFENTANYL
AGONIST -> TARGET
Structure of 2F-MT-45
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
Structure of PIVALOYL FENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of ISOTODESNITAZENE
AGONIST -> TARGET
Emax=94.9 relative to Fentanyl
EC50
Structure of NALMEFENE
INHIBITOR -> TARGET
Structure of U-48800
AGONIST -> TARGET
Has around 7.5-fold the potency of morphine in animal models.
Structure of TIANEPTINE
AGONIST -> TARGET
Atypical. G-protein activation
EC50
Structure of NALOXEGOL
INHIBITOR -> TARGET
Structure of BENZYLFENTANYL
AGONIST -> TARGET
Structure of AT-076
INHIBITOR -> TARGET
ANTAGONIST
Structure of N-DESETHYLETONITAZENE
AGONIST -> TARGET
EC50
Structure of NALDEMEDINE-CARBOXYLIC ACID
INHIBITOR -> TARGET
Structure of 5-AMINOISOTONITAZENE
AGONIST -> TARGET
EC50
Structure of .BETA.-HYDROXYFENTANYL
AGONIST -> TARGET
EC50
Structure of NAPHTHYL-U-47700
AGONIST -> TARGET
Structure of TRIFLUOROFENTANYL
AGONIST -> TARGET
Structure of .ALPHA.-NALOXOL
INHIBITOR -> TARGET
Structure of 4-CHLOROFENTANYL
AGONIST -> TARGET
ED50(mg/kg) = 0.220, Potency ratio to morphine = 1.5, Potency ratio to fentanyl = 0.03
Structure of BENZODIOXOLEFENTANYL
AGONIST -> TARGET
Structure of ETHYLNITAZENE
AGONIST -> TARGET
POTENCY
Structure of 3-METHYLFENTANYL, CIS-
AGONIST -> TARGET
EC50
Structure of 4-PHENYLFENTANYL
AGONIST -> TARGET
Structure of BROMADOL
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
Structure of .ALPHA.-METHYLTHIOFENTANYL
AGONIST -> TARGET
Structure of FENTRANYL
AGONIST -> TARGET
Structure of β-keto-Carfentanil
AGONIST -> TARGET
Lance Ultra cAMP Assay
EC50
Structure of SECOFENTANYL
AGONIST -> TARGET
Structure of ETONITAZENE 6-NITRO ISOMER
AGONIST -> TARGET
POTENCY
Structure of Ohmefentanyl
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
Structure of OXYCODONE
AGONIST -> TARGET
Structure of β-hydroxy-Carfentanil
AGONIST -> TARGET
Lance Ultra cAMP Assay
EC50
Structure of FLUNITAZENE
AGONIST -> TARGET
In vitro data suggest that flunitazene is much less potent than fentanyl. Emax=118% of Fentanyl
EC50
Structure of BUCINNAZINE
AGONIST -> TARGET
Structure of ETONITAZENE
AGONIST -> TARGET
Emax=134% of Fentanyl
EC50
Structure of ETONITAZENE MORPHOLINE ANALOGUE
AGONIST -> TARGET
POTENCY
Structure of TRV-0109662
AGONIST -> TARGET
TRV0109662 is a weak (EC50= 5 mcM) partial agonist of the human mu-opioid receptor.
PARTIAL AGONIST
EC50
Structure of ORP-101
AGONIST -> TARGET
Structure of 1-DIETHYLAMINOETHYL-2-BENZYL-BENZIMIDAZOLE
WEAK AGONIST->TARGET
POTENCY
Structure of ORTHOFLUOROFENTANYL
AGONIST -> TARGET
Structure of CYX-6
AGONIST -> TARGET
Structure of CLONITAZENE
AGONIST -> TARGET
Emax=106 of Fentanyl
EC50
Structure of DAMGO
AGONIST -> TARGET
Ki
Structure of β-Funaltrexamine
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
Structure of 2-METHYLFENTANYL
AGONIST -> TARGET
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 4.0
AGONIST
IC50
Structure of META-METHYLFENTANYL
AGONIST -> TARGET
Structure of AH-7921
AGONIST -> TARGET
Structure of ETONITAZENE N,N-DIMETHYL ANALOGUE
AGONIST -> TARGET
POTENCY
Structure of SAMIDORPHAN
INHIBITOR -> TARGET
Structure of ACETYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of N-DESETHYLISOTONITAZENE
AGONIST -> TARGET
Emax =140% of Fentanyl
EC50
Structure of ETODESNITAZENE
AGONIST -> TARGET
Structure of PROPYLNITAZENE
AGONIST -> TARGET
POTENCY
Structure of THIOFENTANYL
AGONIST -> TARGET
Structure of METENKEFALIN
AGONIST -> TARGET
3-METHYLBUTYRFENTANYL
AGONIST -> TARGET
Structure of NORTILIDINE
AGONIST -> TARGET
Inhibition of forskolin-induced cAMP accumulation.
IC50
Structure of P-BROMOFENTANYL
AGONIST -> TARGET
Rat tail withdrawal test. Morphine ED50 3.15. Fentanyl ED50 0.1 mg/mL
ED50
Structure of ORTHO-METHYLFURANYLFENTANYL
AGONIST -> TARGET
Structure of CYT-1010
AGONIST -> TARGET
Structure of NALBUPHINE
INHIBITOR -> TARGET
Structure of iso-Butanoyl-4-fluorofentanyl
AGONIST -> TARGET
Assumed active
Structure of NOR-NALDEMEDINE
INHIBITOR -> TARGET
Structure of TETRAHYDROFURANYL FENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of SR-17018
AGONIST -> TARGET
Structure of CYCLOPENTYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of N-DESMETHYL-BDPC
AGONIST -> TARGET
Structure of PYRROLE-FENTANYL
AGONIST -> TARGET
Structure of PARA-METHYL ACRYLFENTANYL
AGONIST -> TARGET
Structure of TRAMADOL, (+)-
AGONIST -> TARGET
Structure of BW-942C
AGONIST -> TARGET
Structure of N-PHENYL-N-((1-(2-PHENYLETHYL)PIPERIDIN-4-YL)METHYL)PROPANAMIDE
AGONIST -> TARGET
Structure of OXYCODEGOL
AGONIST -> TARGET
Structure of 4-METHYLPHENETHYLACETYLFENTANYL
AGONIST -> TARGET
Structure of 3-METHYLFURANYLFENTANYL
AGONIST -> TARGET
Structure of PROTODESNITAZENE
AGONIST -> TARGET
EC50
Structure of BISNORTILIDINE
AGONIST -> TARGET
Structure of U-47700
AGONIST -> TARGET
Structure of RR-49
AGONIST -> TARGET
Structure of .ALPHA.-METHYL-METONITAZENE
AGONIST -> TARGET
POTENCY
Structure of p-Fluorofentanyl
AGONIST -> TARGET
EC50
Structure of ELUXADOLINE
AGONIST -> TARGET
Structure of PARA-CHLOROFURANYLFENTANYL
AGONIST -> TARGET
Structure of P-TOLYLFENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of ACETOXYNITAZENE
AGONIST -> TARGET
POTENCY
Structure of BUTONITAZENE
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
Structure of 3-METHYLFENTANYL, (3R,4R)-
AGONIST -> TARGET
Mouse hot plate test. 1516 times more potent than morphine.
ED50
Structure of AP-238
AGONIST -> TARGET
Structure of ETONITAZEPYNE
AGONIST -> TARGET
Structure of Ethyl 4-ANPP
WEAK AGONIST->TARGET
Presumed to be weak agonist.
Structure of SUFENTANIL
AGONIST -> TARGET
10 times more potent than Fentanyl.
Structure of ISOTONITAZENE
AGONIST -> TARGET
Emax 180 of hydromorphone
BIOASSAY (CELLULAR)
EC50
Structure of LOFENTANIL
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
Structure of MORPHINE-6-GLUCURONIDE
AGONIST -> TARGET
Structure of ETOETONITAZENE
AGONIST -> TARGET
POTENCY
Structure of NALDEMEDINE 3-O-.BETA.-D-GLUCURONIDE
INHIBITOR -> TARGET
Structure of 2-METHOXYFENTANYL
AGONIST -> TARGET
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 2.1
AGONIST
IC50
Structure of N-METHYLCARFENTANIL
AGONIST -> TARGET
Structure of ASALHYDROMORPHONE
AGONIST -> TARGET
Structure of 4-FLUOROFURANYL FENTANYL
AGONIST -> TARGET
Structure of T-BUTYLNITAZENE
AGONIST -> TARGET
POTENCY
Structure of METHADONE
INHIBITOR -> TARGET
Structure of META-FLUOROISOBUTYRYL FENTANYL
AGONIST -> TARGET
BINDING
Ki
Structure of Carfentanil
AGONIST -> TARGET
IC50 of Fentanyl= 1.23 NM
IC50
Structure of ORTHO-FLUOROISOBUTYRYL FENTANYL
AGONIST -> TARGET
EC50
Structure of PARA-FLUORO ACRYLFENTANYL
AGONIST -> TARGET
EC50
Structure of PHARAOH FENTANYL
AGONIST -> TARGET
Structure of METONITAZENE
AGONIST -> TARGET
Emax=113% relative to Fentanyl
EC50
Structure of 3-METHYLFENTANYL, (3R,4S)-
AGONIST -> TARGET
Mouse hot plate test. 2600 times more potent than morphine.
ED50
Structure of TREFENTANIL
AGONIST -> TARGET
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
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