Page last updated: 2024-12-11

trk 820

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Description

TRK 820: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6445230
CHEMBL ID267495
CHEMBL ID490665
CHEBI ID136019
SCHEMBL ID7076050
SCHEMBL ID10029279
MeSH IDM0288075

Synonyms (38)

Synonym
trk820
gtpl1651
(e)-n-[(4r,4as,7r,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-7-yl]-3-(furan-3-yl)-n-methylprop-2-enamide
mt-9938
trk-820
nalfurafine
trk 820
CHEBI:136019
CHEMBL267495 ,
bdbm50274347
(2e)-n-[(5r,6r)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(furan-3-yl)-n-methylprop-2-enamide hydrochloride
CHEMBL490665 ,
bdbm50325534
unii-xc41avd567
nalfurafine [inn]
(e)-n-(17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6beta-yl)-3-(furan-3-yl)-n-methylprop-2-enamide
xc41avd567 ,
152657-84-6
2-propenamide, n-((5.alpha.,6.beta.)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl)-3-(3-furanyl)-n-methyl-, (2e)-
nalfurafine [mi]
nalfurafine [who-dd]
XGZZHZMWIXFATA-UEZBDDGYSA-N
17-cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-(n-methyl-trans-3-(3-furyl)acrylamido)morphinan
17-cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[n-methyl-trans-3-(3-furyl)acrylamido]morphinan
SCHEMBL7076050
SCHEMBL10029279
HY-12745
AKOS030526573
(e)-n-[(4r,4as,7r,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]-3-(furan-3-yl)-n-methylprop-2-enamide
DTXSID70905119
DB13471
trk-820 (hydrochloride)
(e)-n-((4r,4as,7r,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6,7,7a-octahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)-3-(furan-3-yl)-n-methylacrylamide ,
Q6960874
EX-A5501
nalfurafin
NCGC00390266-01
IVB ,

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"This open-label study examined the effects and adverse drug reactions (ADRs) of 52-week oral administration of nalfurafine hydrochloride (5 µg/day) in 211 hemodialysis patients with a treatment-resistant itch."( Efficacy and safety of a novel ĸ-agonist for managing intractable pruritus in dialysis patients.
Ebata, T; Kumagai, H; Kurihara, M; Miyasato, K; Muramatsu, T; Nakamoto, H; Suzuki, H; Takamori, K; Yanagita, T, 2012
)
0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
" The permeability of nalfurafine across human P-glycoprotein (P-gp)-expressing LLC-PK1 cells was investigated to evaluate drug-drug interactions (DDI) involving the P-gp efflux transporter of nalfurafine."( Drug-Drug Interactions of a Novel κ-Opioid Receptor Agonist, Nalfurafine Hydrochloride, Involving the P-Glycoprotein.
Ando, A; Miyamoto, Y; Ohzone, Y; Sasago, S, 2016
)
0.43
" Here, we further investigated whether NFF alone (1-10 μg/kg) or in combination with naltrexone (NTX, mu-opioid receptor [MOP-r] antagonist) altered alcohol relapse-like drinking using a mouse alcohol deprivation effect (ADE) paradigm to mimic the relapse episodes in human alcoholics."( Clinically utilized kappa-opioid receptor agonist nalfurafine combined with low-dose naltrexone prevents alcohol relapse-like drinking in male and female mice.
Kreek, MJ; Zhou, Y, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" morphine-induced systemic skin scratching and is more readily absorbed intragastrically than is U-50488H, resulting in high bioavailability in the intragastric route."( Inhibitory effects of TRK-820 on systemic skin scratching induced by morphine in rhesus monkeys.
Endoh, T; Fujiwara, A; Nagase, H; Okano, K; Tanaka, T; Umeuchi, H; Wakasa, Y, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
phenanthrenesAny benzenoid aromatic compound that consists of a phenanthrene skeleton and its substituted derivatives thereof.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorHomo sapiens (human)Ki0.00070.00000.419710.0000AID1877878
Delta-type opioid receptorHomo sapiens (human)Ki0.03650.00000.59789.9300AID1877880
Kappa-type opioid receptorHomo sapiens (human)Ki0.04260.00000.362410.0000AID1255650; AID1877879; AID656903; AID750054
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00060.00000.27869.0000AID502178; AID574377
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mitogen-activated protein kinase 13Homo sapiens (human)EC50 (µMol)0.00520.00521.49585.9000AID1610007
Mitogen-activated protein kinase 3 Homo sapiens (human)EC50 (µMol)0.00050.00050.00530.0100AID1610005
Mitogen-activated protein kinase 1Homo sapiens (human)EC50 (µMol)0.00050.00050.00530.0100AID1610006
Kappa-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00290.00040.00390.0180AID1573415; AID1573419
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.00070.00000.32639.4000AID1167687
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)0.07410.00000.43328.3000AID1167688
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.00050.00000.20671.4454AID1610005
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.02230.00000.22448.9900AID1167689; AID1255660; AID1573413; AID1573417; AID321653
Mitogen-activated protein kinase 12Homo sapiens (human)EC50 (µMol)0.00520.00521.49585.9000AID1610007
Mu-type opioid receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.00050.00000.04930.9320AID1610006
Mitogen-activated protein kinase 11Homo sapiens (human)EC50 (µMol)0.00520.00521.49585.9000AID1610007
Mitogen-activated protein kinase 14Homo sapiens (human)EC50 (µMol)0.00520.00521.51415.9000AID1610007
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (191)

Processvia Protein(s)Taxonomy
response to osmotic stressMitogen-activated protein kinase 13Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 13Homo sapiens (human)
positive regulation of interleukin-6 productionMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to UVMitogen-activated protein kinase 13Homo sapiens (human)
positive regulation of inflammatory responseMitogen-activated protein kinase 13Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to hydrogen peroxideMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to interleukin-1Mitogen-activated protein kinase 13Homo sapiens (human)
cellular response to sorbitolMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to anisomycinMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to sodium arseniteMitogen-activated protein kinase 13Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 13Homo sapiens (human)
positive regulation of macrophage chemotaxisMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of macrophage proliferationMitogen-activated protein kinase 3 Homo sapiens (human)
MAPK cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
DNA-templated transcriptionMitogen-activated protein kinase 3 Homo sapiens (human)
protein phosphorylationMitogen-activated protein kinase 3 Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 3 Homo sapiens (human)
insulin receptor signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
Schwann cell developmentMitogen-activated protein kinase 3 Homo sapiens (human)
phosphorylationMitogen-activated protein kinase 3 Homo sapiens (human)
sensory perception of painMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 3 Homo sapiens (human)
BMP signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of cellular pHMitogen-activated protein kinase 3 Homo sapiens (human)
thyroid gland developmentMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of cyclase activityMitogen-activated protein kinase 3 Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of telomere maintenance via telomeraseMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of stress-activated MAPK cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to amino acid starvationMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to reactive oxygen speciesMitogen-activated protein kinase 3 Homo sapiens (human)
peptidyl-tyrosine autophosphorylationMitogen-activated protein kinase 3 Homo sapiens (human)
ERBB2-ERBB3 signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
outer ear morphogenesisMitogen-activated protein kinase 3 Homo sapiens (human)
myelinationMitogen-activated protein kinase 3 Homo sapiens (human)
signal transduction in response to DNA damageMitogen-activated protein kinase 3 Homo sapiens (human)
response to exogenous dsRNAMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 3 Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
thymus developmentMitogen-activated protein kinase 3 Homo sapiens (human)
modulation of chemical synaptic transmissionMitogen-activated protein kinase 3 Homo sapiens (human)
cartilage developmentMitogen-activated protein kinase 3 Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of cytoskeleton organizationMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of telomerase activityMitogen-activated protein kinase 3 Homo sapiens (human)
Bergmann glial cell differentiationMitogen-activated protein kinase 3 Homo sapiens (human)
face developmentMitogen-activated protein kinase 3 Homo sapiens (human)
lung morphogenesisMitogen-activated protein kinase 3 Homo sapiens (human)
trachea formationMitogen-activated protein kinase 3 Homo sapiens (human)
cardiac neural crest cell development involved in heart developmentMitogen-activated protein kinase 3 Homo sapiens (human)
ERK1 and ERK2 cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
interleukin-1-mediated signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
response to epidermal growth factorMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to mechanical stimulusMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to cadmium ionMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 3 Homo sapiens (human)
caveolin-mediated endocytosisMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of Golgi inheritanceMitogen-activated protein kinase 3 Homo sapiens (human)
xenophagyMitogen-activated protein kinase 3 Homo sapiens (human)
negative regulation of TORC1 signalingMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of telomere cappingMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of xenophagyMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of early endosome to late endosome transportMitogen-activated protein kinase 3 Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of macrophage chemotaxisMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of macrophage proliferationMitogen-activated protein kinase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 1Homo sapiens (human)
protein phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 1Homo sapiens (human)
chemotaxisMitogen-activated protein kinase 1Homo sapiens (human)
DNA damage responseMitogen-activated protein kinase 1Homo sapiens (human)
signal transductionMitogen-activated protein kinase 1Homo sapiens (human)
chemical synaptic transmissionMitogen-activated protein kinase 1Homo sapiens (human)
learning or memoryMitogen-activated protein kinase 1Homo sapiens (human)
insulin receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
Schwann cell developmentMitogen-activated protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
cytosine metabolic processMitogen-activated protein kinase 1Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 1Homo sapiens (human)
androgen receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
regulation of cellular pHMitogen-activated protein kinase 1Homo sapiens (human)
thyroid gland developmentMitogen-activated protein kinase 1Homo sapiens (human)
regulation of protein stabilityMitogen-activated protein kinase 1Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomere maintenance via telomeraseMitogen-activated protein kinase 1Homo sapiens (human)
regulation of stress-activated MAPK cascadeMitogen-activated protein kinase 1Homo sapiens (human)
mammary gland epithelial cell proliferationMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to amino acid starvationMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to reactive oxygen speciesMitogen-activated protein kinase 1Homo sapiens (human)
response to nicotineMitogen-activated protein kinase 1Homo sapiens (human)
ERBB signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
ERBB2-ERBB3 signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
outer ear morphogenesisMitogen-activated protein kinase 1Homo sapiens (human)
myelinationMitogen-activated protein kinase 1Homo sapiens (human)
response to exogenous dsRNAMitogen-activated protein kinase 1Homo sapiens (human)
steroid hormone mediated signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
negative regulation of cell differentiationMitogen-activated protein kinase 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
thymus developmentMitogen-activated protein kinase 1Homo sapiens (human)
progesterone receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
T cell receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
B cell receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 1Homo sapiens (human)
regulation of cytoskeleton organizationMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomerase activityMitogen-activated protein kinase 1Homo sapiens (human)
Bergmann glial cell differentiationMitogen-activated protein kinase 1Homo sapiens (human)
long-term synaptic potentiationMitogen-activated protein kinase 1Homo sapiens (human)
face developmentMitogen-activated protein kinase 1Homo sapiens (human)
lung morphogenesisMitogen-activated protein kinase 1Homo sapiens (human)
trachea formationMitogen-activated protein kinase 1Homo sapiens (human)
labyrinthine layer blood vessel developmentMitogen-activated protein kinase 1Homo sapiens (human)
cardiac neural crest cell development involved in heart developmentMitogen-activated protein kinase 1Homo sapiens (human)
ERK1 and ERK2 cascadeMitogen-activated protein kinase 1Homo sapiens (human)
response to epidermal growth factorMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to cadmium ionMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 1Homo sapiens (human)
caveolin-mediated endocytosisMitogen-activated protein kinase 1Homo sapiens (human)
regulation of Golgi inheritanceMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomere cappingMitogen-activated protein kinase 1Homo sapiens (human)
regulation of early endosome to late endosome transportMitogen-activated protein kinase 1Homo sapiens (human)
cell surface receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
MAPK cascadeMitogen-activated protein kinase 12Homo sapiens (human)
signal transductionMitogen-activated protein kinase 12Homo sapiens (human)
muscle organ developmentMitogen-activated protein kinase 12Homo sapiens (human)
positive regulation of peptidase activityMitogen-activated protein kinase 12Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 12Homo sapiens (human)
signal transduction in response to DNA damageMitogen-activated protein kinase 12Homo sapiens (human)
myoblast differentiationMitogen-activated protein kinase 12Homo sapiens (human)
negative regulation of cell cycleMitogen-activated protein kinase 12Homo sapiens (human)
positive regulation of muscle cell differentiationMitogen-activated protein kinase 12Homo sapiens (human)
regulation of cell cycleMitogen-activated protein kinase 12Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 12Homo sapiens (human)
positive regulation of erythrocyte differentiationMitogen-activated protein kinase 11Homo sapiens (human)
osteoblast differentiationMitogen-activated protein kinase 11Homo sapiens (human)
positive regulation of gene expressionMitogen-activated protein kinase 11Homo sapiens (human)
stress-activated protein kinase signaling cascadeMitogen-activated protein kinase 11Homo sapiens (human)
positive regulation of interleukin-12 productionMitogen-activated protein kinase 11Homo sapiens (human)
p38MAPK cascadeMitogen-activated protein kinase 11Homo sapiens (human)
positive regulation of muscle cell differentiationMitogen-activated protein kinase 11Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 11Homo sapiens (human)
cardiac muscle cell proliferationMitogen-activated protein kinase 11Homo sapiens (human)
negative regulation of cardiac muscle cell proliferationMitogen-activated protein kinase 11Homo sapiens (human)
bone developmentMitogen-activated protein kinase 11Homo sapiens (human)
cellular response to interleukin-1Mitogen-activated protein kinase 11Homo sapiens (human)
cellular response to UV-BMitogen-activated protein kinase 11Homo sapiens (human)
cellular senescenceMitogen-activated protein kinase 11Homo sapiens (human)
cellular response to virusMitogen-activated protein kinase 11Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 11Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipopolysaccharideMitogen-activated protein kinase 14Homo sapiens (human)
DNA damage checkpoint signalingMitogen-activated protein kinase 14Homo sapiens (human)
cell morphogenesisMitogen-activated protein kinase 14Homo sapiens (human)
cartilage condensationMitogen-activated protein kinase 14Homo sapiens (human)
angiogenesisMitogen-activated protein kinase 14Homo sapiens (human)
osteoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
placenta developmentMitogen-activated protein kinase 14Homo sapiens (human)
response to dietary excessMitogen-activated protein kinase 14Homo sapiens (human)
chondrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusMitogen-activated protein kinase 14Homo sapiens (human)
glucose metabolic processMitogen-activated protein kinase 14Homo sapiens (human)
regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 14Homo sapiens (human)
chemotaxisMitogen-activated protein kinase 14Homo sapiens (human)
signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor protein serine/threonine kinase signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
skeletal muscle tissue developmentMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of gene expressionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myotube differentiationMitogen-activated protein kinase 14Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 14Homo sapiens (human)
fatty acid oxidationMitogen-activated protein kinase 14Homo sapiens (human)
platelet activationMitogen-activated protein kinase 14Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 14Homo sapiens (human)
osteoclast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated protein kinase signaling cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cyclase activityMitogen-activated protein kinase 14Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
response to muramyl dipeptideMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of interleukin-12 productionMitogen-activated protein kinase 14Homo sapiens (human)
response to insulinMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of hippo signalingMitogen-activated protein kinase 14Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusMitogen-activated protein kinase 14Homo sapiens (human)
response to muscle stretchMitogen-activated protein kinase 14Homo sapiens (human)
p38MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of protein import into nucleusMitogen-activated protein kinase 14Homo sapiens (human)
signal transduction in response to DNA damageMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of erythrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
glucose importMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of glucose importMitogen-activated protein kinase 14Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
stem cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
striated muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationMitogen-activated protein kinase 14Homo sapiens (human)
bone developmentMitogen-activated protein kinase 14Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipoteichoic acidMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to ionizing radiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to UV-BMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of brown fat cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular senescenceMitogen-activated protein kinase 14Homo sapiens (human)
stress-induced premature senescenceMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to virusMitogen-activated protein kinase 14Homo sapiens (human)
regulation of synaptic membrane adhesionMitogen-activated protein kinase 14Homo sapiens (human)
regulation of cytokine production involved in inflammatory responseMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast fusionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processMitogen-activated protein kinase 14Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
protein serine/threonine kinase activityMitogen-activated protein kinase 13Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 13Homo sapiens (human)
protein bindingMitogen-activated protein kinase 13Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 13Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 13Homo sapiens (human)
phosphotyrosine residue bindingMitogen-activated protein kinase 3 Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 3 Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 3 Homo sapiens (human)
protein bindingMitogen-activated protein kinase 3 Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 3 Homo sapiens (human)
phosphatase bindingMitogen-activated protein kinase 3 Homo sapiens (human)
identical protein bindingMitogen-activated protein kinase 3 Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 3 Homo sapiens (human)
DNA-binding transcription factor bindingMitogen-activated protein kinase 3 Homo sapiens (human)
phosphotyrosine residue bindingMitogen-activated protein kinase 1Homo sapiens (human)
DNA bindingMitogen-activated protein kinase 1Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
protein bindingMitogen-activated protein kinase 1Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 1Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
phosphatase bindingMitogen-activated protein kinase 1Homo sapiens (human)
identical protein bindingMitogen-activated protein kinase 1Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
magnesium ion bindingMitogen-activated protein kinase 12Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 12Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 12Homo sapiens (human)
protein bindingMitogen-activated protein kinase 12Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 12Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 12Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 11Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 11Homo sapiens (human)
protein bindingMitogen-activated protein kinase 11Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 11Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 11Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 14Homo sapiens (human)
enzyme bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein phosphatase bindingMitogen-activated protein kinase 14Homo sapiens (human)
mitogen-activated protein kinase p38 bindingMitogen-activated protein kinase 14Homo sapiens (human)
NFAT protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (42)

Processvia Protein(s)Taxonomy
cytosolMitogen-activated protein kinase 13Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 13Homo sapiens (human)
nucleusMitogen-activated protein kinase 13Homo sapiens (human)
nucleusMitogen-activated protein kinase 3 Homo sapiens (human)
nuclear envelopeMitogen-activated protein kinase 3 Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 3 Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 3 Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 3 Homo sapiens (human)
early endosomeMitogen-activated protein kinase 3 Homo sapiens (human)
late endosomeMitogen-activated protein kinase 3 Homo sapiens (human)
endoplasmic reticulum lumenMitogen-activated protein kinase 3 Homo sapiens (human)
Golgi apparatusMitogen-activated protein kinase 3 Homo sapiens (human)
cytosolMitogen-activated protein kinase 3 Homo sapiens (human)
cytoskeletonMitogen-activated protein kinase 3 Homo sapiens (human)
plasma membraneMitogen-activated protein kinase 3 Homo sapiens (human)
caveolaMitogen-activated protein kinase 3 Homo sapiens (human)
focal adhesionMitogen-activated protein kinase 3 Homo sapiens (human)
pseudopodiumMitogen-activated protein kinase 3 Homo sapiens (human)
glutamatergic synapseMitogen-activated protein kinase 3 Homo sapiens (human)
nucleusMitogen-activated protein kinase 3 Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 3 Homo sapiens (human)
extracellular regionMitogen-activated protein kinase 1Homo sapiens (human)
nucleusMitogen-activated protein kinase 1Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 1Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 1Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 1Homo sapiens (human)
early endosomeMitogen-activated protein kinase 1Homo sapiens (human)
late endosomeMitogen-activated protein kinase 1Homo sapiens (human)
endoplasmic reticulum lumenMitogen-activated protein kinase 1Homo sapiens (human)
Golgi apparatusMitogen-activated protein kinase 1Homo sapiens (human)
centrosomeMitogen-activated protein kinase 1Homo sapiens (human)
cytosolMitogen-activated protein kinase 1Homo sapiens (human)
cytoskeletonMitogen-activated protein kinase 1Homo sapiens (human)
plasma membraneMitogen-activated protein kinase 1Homo sapiens (human)
caveolaMitogen-activated protein kinase 1Homo sapiens (human)
focal adhesionMitogen-activated protein kinase 1Homo sapiens (human)
pseudopodiumMitogen-activated protein kinase 1Homo sapiens (human)
azurophil granule lumenMitogen-activated protein kinase 1Homo sapiens (human)
synapseMitogen-activated protein kinase 1Homo sapiens (human)
mitotic spindleMitogen-activated protein kinase 1Homo sapiens (human)
ficolin-1-rich granule lumenMitogen-activated protein kinase 1Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 1Homo sapiens (human)
nucleusMitogen-activated protein kinase 1Homo sapiens (human)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
nucleoplasmMitogen-activated protein kinase 12Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 12Homo sapiens (human)
cytosolMitogen-activated protein kinase 12Homo sapiens (human)
nucleusMitogen-activated protein kinase 12Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 12Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 11Homo sapiens (human)
cytosolMitogen-activated protein kinase 11Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 11Homo sapiens (human)
nucleusMitogen-activated protein kinase 11Homo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
spindle poleMitogen-activated protein kinase 14Homo sapiens (human)
extracellular regionMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 14Homo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
nuclear speckMitogen-activated protein kinase 14Homo sapiens (human)
secretory granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
glutamatergic synapseMitogen-activated protein kinase 14Homo sapiens (human)
ficolin-1-rich granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID1255660Agonist activity at kappa opioid receptor in human HEK293 cells after 30 mins by [35S]GTPgammaS binding assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1167687Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID321655Selectivity for human kappa opioid receptor over rat mu opioid receptor2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
AID502177Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
AID1255652Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID656903Binding affinity to kappa opioid receptor2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
AID1573416Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Western blot analysis relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID1885877Toxicity in ICR mouse assessed as reduction in time stayed in rod at 0.006 to 0.02 mg/kg, ip for 20 mins by rotarod test2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
AID1573418Agonist activity at FLAG-tagged human kappa opioid receptor expressed in HEK293 cells assessed as increase in beta-arrestin mediated p38 phosphorylation after 5 mins by Western blot analysis relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID574377Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
AID502180Selectivity ratio of Ki for mu opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
AID750054Binding affinity to kappa opioid receptor (unknown origin)2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton having a 7-amide side chain and their pharmacologies.
AID1255662Intrinsic activity at kappa opioid receptor in human HEK293 cells at 100 nM after 30 mins by [35S]GTPgammaS binding assay relative to U-695932015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1877882Selectivity index, ratio of Ki for displacement of [3H]U-69-593 from human DOR expressed in HEK293 cell membrane to displacement of [3H]DPDPE from human KOR expressed in HEK293 cell membrane2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
AID1722000Analgesic activity in OX1R knock out mouse assessed as increase in wheel running activity at 4 to 10 ug/kg2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine.
AID574381Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain to Ki for mu opioid receptor in guinea pig forebrain2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
AID1573417Agonist activity at FLAG-tagged human kappa opioid receptor expressed in HEK293 cells assessed as increase in beta-arrestin mediated p38 phosphorylation after 5 mins by Western blot analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID1167683Displacement of [3H]DAMGO from mu opioid receptor in mouse brain membranes without cerebellum2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID1573413Agonist activity at FLAG-tagged human kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Western blot analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID1722004Toxicity in mouse assessed as conditioned place aversion at 10 to 40 microg/kg, sc2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine.
AID1877881Selectivity index, ratio of Ki for displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membrane to displacement of [3H]DPDPE from human KOR expressed in HEK293 cell membrane2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
AID1573415Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Western blot analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID1573414Agonist activity at FLAG-tagged human kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Western blot analysis relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID1255650Binding affinity to kappa opioid receptor (unknown origin)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID502178Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
AID574379Selectivity ratio of Ki for mu opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
AID1573419Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in beta-arrestin mediated p38 phosphorylation after 5 mins by Western blot analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID1167686Selectivity ratio of Ki for mu opioid receptor in mouse brain membranes without cerebellum to Ki for kappa opioid receptor in guinea pig cerebellum2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID1167691Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to SNC802014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID574380Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
AID1877879Displacement of [3H]DPDPE from human KOR expressed in HEK293 cell membrane2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
AID1610007Inhibition of p38 phosphorylation (unknown origin)2019European journal of medicinal chemistry, Dec-01, Volume: 183Progress in the development of more effective and safer analgesics for pain management.
AID574382Antinociceptive activity in sc dosed mouse assessed as effect on acetic acid-induced writhing2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
AID1721999Analgesic activity in OX1R knock out mouse assessed as increase in wheel running activity at 40 ug/kg2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine.
AID1167688Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID1877880Displacement of [3H]U-69-593 from human DOR expressed in HEK293 cell membrane2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
AID1167689Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID1461556Antimicrobial activity against Trichomonas vaginalis after 48 hrs by neutral red staining based invert microscopic analysis2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives.
AID1877878Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membrane2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
AID1255651Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1167684Displacement of [3H]DPDPE from delta opioid receptor in mouse brain membranes without cerebellum2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID502179Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
AID1167685Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID1722005Toxicity in dual OX1/2R knock out mouse assessed as increase in conditioned place aversion at 10 to 40 microg/kg, sc2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine.
AID574378Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
AID574376Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
AID1255653Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
AID1610005Inhibition of ERK1 phosphorylation (unknown origin)2019European journal of medicinal chemistry, Dec-01, Volume: 183Progress in the development of more effective and safer analgesics for pain management.
AID1573420Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in beta-arrestin mediated p38 phosphorylation after 5 mins by Western blot analysis relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID502181Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
AID1167690Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to DAMGO2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID1721997Dissociation constant, pKa of compound2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine.
AID1610006Inhibition of ERK2 phosphorylation (unknown origin)2019European journal of medicinal chemistry, Dec-01, Volume: 183Progress in the development of more effective and safer analgesics for pain management.
AID321653Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
AID1167692Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to U-695932014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
AID1346329Human kappa receptor (Opioid receptors)2005The Journal of pharmacology and experimental therapeutics, Jan, Volume: 312, Issue:1
Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (120)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (2.50)18.2507
2000's38 (31.67)29.6817
2010's50 (41.67)24.3611
2020's29 (24.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.99

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index21.99 (24.57)
Research Supply Index4.85 (2.92)
Research Growth Index5.20 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (3.25%)5.53%
Reviews17 (13.82%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other102 (82.93%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]