Page last updated: 2024-11-04

levallorphan

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

dextrallorphan: RN given refers to (9alpha,13alpha,14alpha)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Levallorphan: An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3912
CHEMBL ID608539
SCHEMBL ID209271
MeSH IDM0012429
PubMed CID5359371
CHEMBL ID1254682
CHEBI ID6431
SCHEMBL ID34060
MeSH IDM0012429

Synonyms (72)

Synonym
levo-3-hydroxy-n-allyl morphinan
morphinan-3-ol, 17-allyl-
ro-1-7700
n-allyl-3-hydroxymorphinan
(-)-3-hydroxy-n-allylmorphinan
morphinan, 17-allyl-3-hydroxy-
l-n-allyl-3-hydroxymorphinan
morphinan-3-ol, 17-(2-propenyl)-
dextrallorphan
L001162
CHEMBL608539
nsc_9036
cas_152-02-3
bdbm92849
SCHEMBL209271
OZYUPQUCAUTOBP-UHFFFAOYSA-N
levallorphan tartrate (salt/mix)
lorfan (salt/mix)
17-prop-2-enyl-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-ol
Q5268487
1,3-dioxolan-2-one; ethylene carbonate; ethylene glycol carbonate
DTXSID80859295
17-(prop-2-en-1-yl)morphinan-3-ol
17-prop-2-en-1-ylmorphinan-3-ol
lorfan
levalorfano [inn-spanish]
morphinan-3-ol, 17-allyl-, (-)-
levallorphanum [inn-latin]
hsdb 2148
naloxiphan
levallorphane [inn-french]
einecs 205-799-1
17-allylmorphinan-3-ol
levallorphan [inn:ban]
levallofano [dcit]
C07069
152-02-3
levallorphan
DB00504
NCGC00162247-02
17-allyl-(1r,9r)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-ol( levallorphan)
17-allyl-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-ol (levallorphan)
(levallorphan)17-allyl-(1r,9r)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-ol
levallofano
353613bu4u ,
levalorfano
levallorphane
levallorphanum
unii-353613bu4u
bdbm50326673
chebi:6431 ,
CHEMBL1254682 ,
tox21_112005
cas-152-02-3
dtxsid9023205 ,
dtxcid703205
levallorphan [hsdb]
levallorphan [who-dd]
levallorphan [mi]
levallorphan [inn]
gtpl7209
SCHEMBL34060
NCGC00162247-06
tox21_112005_1
(1r,9r,10r)-17-(prop-2-en-1-yl)-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2(7),3,5-trien-4-ol
mcl 113; n-allyl-3-hydroxymorphinan
Q6534827
(1r,9r,10r)-17-prop-2-enyl-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-ol
(-)-17-allylmorphinan-3-ol
(a^?-17-allylmorphinan-3-ol
EN300-19767758
AKOS040752523

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Maternal adverse effects of Pethilorfan were generally mild and transient."( Safety and efficacy of a combination of pethidine and levallorphan for pain relief during labor: An observational study.
Kinugasa, M; Miyake, M; Tamai, H; Tamura, M, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Physical dependence on phenobarbital and diazepam was produced using the same dosage schedules as with morphine."( Physical dependence on morphine, phenobarbital and diazepam in rats by drug-admixed food ingestion.
Suzuki, T; Tagashira, E; Yanaura, S, 1975
)
0.25
" We generated dose-response curves for centrally and peripherally administered SR58002C, a "newer" quaternary opioid antagonist purported to have high peripheral selectivity, on drinking in 23."( Central and peripheral injection of quaternary antagonist, SR58002C, reduces drinking.
Calcagnetti, DJ; Fanselow, MS; Helmstetter, FJ, 1987
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
morphinane alkaloidAn isoquinoline alkaloid based on a morphinan skeleton and its substituted derivatives.
[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]

Pathways (1)

PathwayProteinsCompounds
Levallorphan Action Pathway3111

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency21.51370.002541.796015,848.9004AID1347395; AID1347398
TDP1 proteinHomo sapiens (human)Potency4.73180.000811.382244.6684AID686978
AR proteinHomo sapiens (human)Potency27.20510.000221.22318,912.5098AID743042; AID743054; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency33.49150.000657.913322,387.1992AID1259377
estrogen nuclear receptor alphaHomo sapiens (human)Potency31.26310.000229.305416,493.5996AID743075; AID743079; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency1.09640.00108.379861.1304AID1645840
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency29.84930.000323.4451159.6830AID743065; AID743067
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AcetylcholinesteraseElectrophorus electricus (electric eel)Ki12.00000.00121.25638.9000AID514203
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00080.00030.38877.0000AID149041
Mu-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00080.00010.887410.0000AID149041
Kappa-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00080.00050.36987.0000AID149041
Mu-type opioid receptorHomo sapiens (human)Ki0.00120.00000.419710.0000AID603169; AID603170; AID603171
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki12.00000.00000.20186.4240AID514203
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID23717Partition coefficient (logP)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor.
AID151584Binding constant for the agonist state was measured for its ability to displace [3H]naloxone from opioid mu 1 receptor buffered homogenate of rat brain membranes1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor.
AID151914Binding constant for the antagonist state was measured for its ability to displace [3H]naloxone from opioid mu 1 receptor buffered homogenate of rat brain membranes1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID148471Inhibition of [3H]DADLE binding to opioid receptor1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID234027The sodium index is the ratio of the IC50 value for the inhibition of [3H]naloxone binding to homogenates of rat brain minus cerebellum in presence of 100 mM of NaCl.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity.
AID603171Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Generation of novel radiolabeled opiates through site-selective iodination.
AID135326BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID514203Inhibition of electric eel AChE by Ellman's method2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
AID179385Concentration of drug required to inhibit the stereospecific binding of [3H]-naloxone (5 nM) to homogenates of rat brain minus cerebellum in the absence of 100 mM NaCl1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity.
AID603170Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Generation of novel radiolabeled opiates through site-selective iodination.
AID149041Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID603169Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Generation of novel radiolabeled opiates through site-selective iodination.
AID148472Inhibition of [3H]fluadom binding to opioid receptor1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID179386Concentration of drug required to inhibit the stereospecific binding of [3H]naloxone (5 nM) to homogenates of rat brain minus cerebellum in the presence of 100 mM NaCl1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity.
AID232429Ratio of inhibition of binding to opioid receptor in the presence and absence of NaCl1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID620063Displacement of [3H]-dihydromorphine from mu opioid receptor in rat cerebral cortex by liquid scintillation counting2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Derivatives of pyrrolo[3,4-d]pyridazinone, a new class of analgesic agents.
AID1346364Human mu receptor (Opioid receptors)2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Generation of novel radiolabeled opiates through site-selective iodination.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (397)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990358 (90.18)18.7374
1990's19 (4.79)18.2507
2000's5 (1.26)29.6817
2010's8 (2.02)24.3611
2020's7 (1.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 36.76

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 Index36.76 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index44.79 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (36.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials13 (3.15%)5.53%
Reviews0 (0.00%)6.00%
Reviews9 (2.18%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies4 (0.97%)4.05%
Observational0 (0.00%)0.25%
Observational1 (0.24%)0.25%
Other10 (100.00%)84.16%
Other386 (93.46%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]