Page last updated: 2024-11-11

nalfurafine hydrochloride

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Cross-References

ID SourceID
PubMed CID6918287
SCHEMBL ID19856501
MeSH IDM0489682

Synonyms (37)

Synonym
remitch ,
nalfurafine hydrochloride
nalfurafine hydrochloride (jan/usan)
D06405
152658-17-8
(e)-n-(17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6beta-yl)-3-(furan-3-yl)-n-methylprop-2-enamide monohydrochloride
nalfurafine hydrochloride [usan]
2-propenamide, n-((5alpha,6beta)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl)-3-(3-furanyl)-n-methyl-, monohydrochloride, (2e)-
(-)-17-(cyclopropylmethyl-3,14 beta-dihydroxy-4,5 alpha-epoxy-6 beta-(n-methyl-trans-3-(3-furyl)acrylamido)morphinan hydrochloride
nopicor
nalfurafine hcl
25cc4n0p8j ,
unii-25cc4n0p8j
nalfurafine hydrochloride [usan:jan]
ac 820
(e)-n-[17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6beta-yl]-3-(furan-3-yl)-n-methylprop-2-enamide monohydrochloride
nalfurafine hydrochloride [jan]
2-propenamide, n-((5.alpha.,6.beta.)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl)-3-(3-furanyl)-n-methyl-, monohydrochloride, (2e)-
nalfurafine hydrochloride [who-dd]
nalfurafine hydrochloride [mart.]
nalfurafine hydrochloride [mi]
(-)-17-(cyclopropylmethyl-3,14.beta.-dihydroxy-4,5.alpha.-epoxy-6.beta.-(n-methyl-trans-3-(3-furyl)acrylamid)morphinan hydrochloride
17-cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[n-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride
DJSFYNINGIMKAG-FQJQBBMWSA-N
DTXSID70426071
SCHEMBL19856501
HY-12745A
nalfurafine (hydrochloride)
AC-32785
AKOS030526574
trk-820 hydrochloride
BCP15625
EX-A2892
2-propenamide,n-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-n-methyl-, monohydrochloride, (2e)-
Q27253946
(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;hydrochloride
F85198
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Orexin receptor type 1Homo sapiens (human)Ki0.25000.00030.28763.1623AID1426493
Mu-type opioid receptorHomo sapiens (human)Ki0.00600.00000.419710.0000AID1426492
Delta-type opioid receptorHomo sapiens (human)Ki0.69300.00000.59789.9300AID1426495
Kappa-type opioid receptorHomo sapiens (human)Ki0.00020.00000.362410.0000AID1426496
Mu-type opioid receptorMus musculus (house mouse)Ki0.02590.00000.12281.3000AID657051; AID657052
[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)
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.00170.00000.32639.4000AID1487647
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.00000.00000.22448.9900AID1487646; AID724712
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)Ke0.04160.00010.14726.1080AID389661
Kappa-type opioid receptorMus musculus (house mouse)Ke0.00020.00000.32251.5510AID389663
Mu-type opioid receptorMus musculus (house mouse)Ke7.02400.00020.02330.0554AID389659; AID389660
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (55)

Processvia Protein(s)Taxonomy
neuropeptide signaling pathwayOrexin receptor type 1Homo sapiens (human)
chemical synaptic transmissionOrexin receptor type 1Homo sapiens (human)
feeding behaviorOrexin receptor type 1Homo sapiens (human)
regulation of cytosolic calcium ion concentrationOrexin receptor type 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeOrexin receptor type 1Homo sapiens (human)
cellular response to hormone stimulusOrexin receptor type 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityOrexin receptor type 1Homo sapiens (human)
protein bindingOrexin receptor type 1Homo sapiens (human)
orexin receptor activityOrexin receptor type 1Homo sapiens (human)
peptide hormone bindingOrexin receptor type 1Homo sapiens (human)
peptide bindingOrexin receptor type 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
plasma membraneOrexin receptor type 1Homo sapiens (human)
synapseOrexin receptor type 1Homo sapiens (human)
plasma membraneOrexin receptor type 1Homo sapiens (human)
plasma membraneKappa-type opioid receptorMus musculus (house mouse)
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)
plasma membraneMu-type opioid receptorMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (63)

Assay IDTitleYearJournalArticle
AID657055Selectivity ratio of Ki for mouse delta opioid receptor to Ki for guinea pig kappa opioid receptor2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
AID673191Displacement of [3H]DAMGO from mu opioid receptor in mouse cerebellum2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
AID389665Antinociceptive activity in sc dosed mouse assessed as inhibition of acetic acid-induced writhing administered 15 mins before acetic acid challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID724711Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay relative to control2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
AID1245662Therapeutic index, ratio of ED50 for induction of sedation in ICR mouse by spontaneous locomotor activity test to ED50 for antinociceptive activity in ICR mouse by acetic acid abdominal constriction test2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID389682Selectivity ratio of Ke for mu opioid receptor in guinea pig ileum to Ke for kappa opioid receptor in guinea pig ileum2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID1487646Agonist activity at kappa opioid receptor (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Discovery of highly selective κ-opioid receptor agonists: 10α-Hydroxy TRK-820 derivatives.
AID603727Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain homogenate to Ki for kappa opioid receptor in guinea pig cerebellum homogenate2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
AID657054Selectivity ratio of Ki for mouse mu opioid receptor to Ki for guinea pig kappa opioid receptor2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
AID718963Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum membranes2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
AID718965Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes without cerebellum2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
AID1426493Antagonist activity at human OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular calcium level preincubated for 15 mins followed by orexin A addition by Fura-2-AM dye based fluorescence assay2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID603730Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain homogenate by scintillation counting2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
AID718962Selectivity ratio of Ki for mu opioid receptor in mouse whole brain membranes without cerebellum to Ki for kappa opioid receptor in guinea pig cerebellum membranes2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
AID389663Equilibrium constant, ratio of IC50 for kappa opioid receptor in ddy mouse vas deferens in presence of 10 nM nor-BNI to IC50 for kappa opioid receptor in ddy mouse vas deferens2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID389661Equilibrium constant, ratio of IC50 for delta opioid receptor in ddy mouse vas deferens in presence of 10 nM Naltrindole to IC50 for delta opioid receptor in ddy mouse vas deferens2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID389673Equilibrium constant, ratio of IC50 for mu opioid receptor in guinea pig ileum in presence of 100 nM Naloxone to IC50 for mu opioid receptor in guinea pig ileum2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID724714Selectivity ratio of Ki for mu opioid receptor in mouse whole brain membranes without cerebellum to Ki for kappa opioid receptor in guinea pig cerebellum2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
AID1245656Selectivity index, ratio of Ki for MOR in guinea pig cerebellum membranes to Ki for KOR in mouse whole brain membranes without cerebellum2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID1426494Antagonist activity at human OX2R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular calcium level preincubated for 15 mins followed by orexin A addition by Fura-2-AM dye based fluorescence assay2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID1245661Induction of sedation in ICR mouse by spontaneous locomotor activity test2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID1426492Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes by micro-beta scintillation counting method2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID1426497Solubility of the compound in water2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID389656Antinociceptive activity in sc dosed kappa opioid receptor antagonist nor-BNI treated mouse assessed as inhibition of acetic acid-induced writhing administered 15 mins before acetic acid challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID718961Selectivity ratio of Ki for delta opioid receptor in mouse whole brain membranes without cerebellum to Ki for kappa opioid receptor in guinea pig cerebellum membranes2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
AID1245653Displacement of [3H]DAMGO from MOR in guinea pig cerebellum membranes2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID1426498Solubility of the compound in saline2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID1245657Selectivity index, ratio of Ki for DOR in mouse whole brain membranes without cerebellum to Ki for KOR in mouse whole brain membranes without cerebellum2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID657052Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
AID389667Antinociceptive activity in po dosed mouse assessed as inhibition of acetic acid-induced writhing administered 15 mins before acetic acid challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID1245654Displacement of [3H]DPDPE from DOR in mouse whole brain membranes without cerebellum2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID724712Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
AID1426499Selectivity index, ratio of IC50 for human OX2R expressed in CHOK1 cells to IC50 for human OX1R expressed in CHOK1 cells2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID724716Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain membranes without cerebellum after 1 hr by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
AID389671Equilibrium constant, ratio of IC50 for kappa opioid receptor in guinea pig ileum in presence of 10 nM nor-BNI to IC50 for kappa opioid receptor in guinea pig ileum2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID1487647Agonist activity at mu opioid receptor (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Discovery of highly selective κ-opioid receptor agonists: 10α-Hydroxy TRK-820 derivatives.
AID389678Selectivity ratio of Ke for mu opioid receptor in ddy mouse vas deferens to Ke for kappa opioid receptor in ddy mouse vas deferens2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID724713Selectivity ratio of Ki for delta opioid receptor in mouse whole brain membranes without cerebellum to Ki for kappa opioid receptor in guinea pig cerebellum2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
AID1426495Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cell membranes by micro-beta scintillation counting method2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID673193Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
AID1245655Displacement of [3H]U69,593 from KOR in mouse whole brain membranes without cerebellum2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID389660Equilibrium constant, ratio of IC50 for mu opioid receptor in ddy mouse vas deferens in presence of 100 nM naloxone to IC50 for mu opioid receptor in ddy mouse vas deferens2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID603729Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain homogenate by scintillation counting2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
AID724715Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum after 1 hr by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
AID603728Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
AID603731Selectivity ratio of Ki for mu opioid receptor in guinea pig forebrain homogenate to Ki for kappa opioid receptor in guinea pig cerebellum homogenate2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
AID657051Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
AID657053Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
AID389681Antinociceptive activity in sc dosed mu opioid receptor antagonist naloxone treated mouse assessed as inhibition of acetic acid-induced writhing administered 15 mins before acetic acid challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID1426496Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membranes by micro-beta scintillation counting method2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
AID673192Displacement of [3H]DPDPE from delta opioid receptor in mouse cerebellum2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
AID1245660Antinociceptive activity in ICR mouse assessed as reduction in acetic acid-induced abdominal writhing dosed subcutaneously 15 mins before acetic acid challenge2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
AID724717Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes without cerebellum after 1 hr by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
AID718964Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain membranes without cerebellum2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
AID389680Antinociceptive activity in sc dosed delta opioid receptor antagonist Naloxone treated mouse assessed as inhibition of acetic acid-induced writhing administered 15 mins before acetic acid challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID389669Inhibition of acetic acid-induced writhing in sc dosed mouse up to 180 mins administered 15 mins before acetic acid challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID389668Ratio of ED50 for acetic acid-induced writhing in po dosed mouse to ED50 for acetic acid-induced writhing in sc dosed mouse2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID389657Agonist activity at kappa opioid receptor in ddy mouse vas deferens assessed as inhibition of electric stimulation-induced contraction2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID389655Antinociceptive activity in po dosed mouse by tail flick test2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID673195Selectivity ratio of Ki for delta opioid receptor in mouse cerebellum to Ki for kappa opioid receptor in guinea pig cerebellum2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
AID389659Equilibrium constant, ratio of IC50 for mu opioid receptor in ddy mouse vas deferens in presence of 30 nM naloxone to IC50 for mu opioid receptor in ddy mouse vas deferens2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID389670Agonist activity at kappa opioid receptor in guinea pig ileum assessed as inhibition of electric stimulation-induced contraction2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
AID673194Selectivity ratio of Ki for mu opioid receptor in mouse cerebellum to Ki for kappa opioid receptor in guinea pig cerebellum2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (11.11)29.6817
2010's8 (88.89)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.53

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index44.53 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index5.53 (4.65)
Search Engine Demand Index60.33 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (44.53)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]