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oxymorphindole

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

Description

oxymorphindole: no other info avail 9/91 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5491897
CHEMBL ID401093
CHEMBL ID557978
MeSH IDM0191780

Synonyms (21)

Synonym
111469-88-6
oxymorphindole
CHEMBL401093 ,
bdbm50218796
oxymorphindole chloride
22-methyl-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5(10),6,8,15(25),16,18-heptaene-2,16-diol
CHEMBL557978 ,
22-methyl-(2s,13r)-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5(10),6,8,15(25),16,18-heptaene-2,16-diol(hcl0.5h2o) (oxymorphindole, omi)
bdbm50221416
4,8-methanobenzofuro(2,3-a)pyrido(4,3-b)carbazole-1,8a(9h)-diol, 5,6,7,8,14,14b-hexahydro-7-methyl-, (4bs,8r,8as,14br)-
nih 10842
4,8-methanobenzofuro(2,3-a)pyrido(4,3-b)carbazole-1,8a(9h)-diol, 5,6,7,8,14,14b-hexahydro-7-methyl-, (8r-(4bs*,8alpha,8abeta,14bbeta))-
7-methyl-5,6,7,8,14,14b-hexahydro-4,8-methano[1]benzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol
DTXSID80912172
(1s,2s,13r,21r)-22-methyl-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15,17,19(25)-heptaene-2,16-diol
B85P9S9T5L
4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol, 5,6,7,8,14,14b-hexahydro-7-methyl-, (4bs,8r,8as,14br)-
4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol, 5,6,7,8,14,14b-hexahydro-7-methyl-, [8r-(4bs*,8alpha,8abeta,14bbeta)]-
nih-10842
(4bs,8r,8as,14br)-5,6,7,8,14,14b-hexahydro-7-methyl-4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol
(1s,2s,13r,21r)-22-methyl-14-oxa-11,22-diazaheptacyclo[13.9.1.0{1,13}.0{2,21}.0{4,12}.0{5,10}.0{19,25}]pentacosa-4(12),5(10),6,8,15,17,19(25)-heptaene-2,16-diol

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves for each route of administration and each nociceptive test were generated, and analgesic synergy was assessed by isobolographic analysis."( Combination of a δ-opioid Receptor Agonist and Loperamide Produces Peripherally-mediated Analgesic Synergy in Mice.
Akgün, E; Bruce, DJ; Fairbanks, CA; Kitto, KF; Lazzaroni, S; Peterson, CD; Portoghese, PS; Wilcox, GL, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)Ki0.00080.00000.53939.4000AID149074; AID149075
Kappa-type opioid receptorMus musculus (house mouse)Ki0.07700.00030.35942.7500AID148317
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.51230.00000.38458.6000AID151151; AID152379
Mu-type opioid receptorHomo sapiens (human)Ki0.23400.00000.419710.0000AID150841; AID309541
Delta-type opioid receptorHomo sapiens (human)Ki0.00110.00000.59789.9300AID148220; AID309542
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.39500.00000.20186.4240AID149544
Kappa-type opioid receptorHomo sapiens (human)Ki0.45550.00000.362410.0000AID147987; AID309543
Mu-type opioid receptorMus musculus (house mouse)Ki0.66100.00000.12281.3000AID151151
[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)Ke0.00500.00010.14726.1080AID148810
Delta-type opioid receptorRattus norvegicus (Norway rat)Activity0.00650.00000.11931.2200AID310939
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ke0.16700.00000.03891.1570AID148835
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ke0.11100.00000.01590.0430AID150010
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

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)
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 (12)

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)
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 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 (60)

Assay IDTitleYearJournalArticle
AID235352Selectivity ratio (Ki value towards kappa receptor compared to that of delta receptor).2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
AID310938Agonist activity at rat delta opioid receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to BW373U862007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity.
AID152379Displacement of [3H]DAMGO at mu-opioid receptor2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
AID148220Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes.2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID147964Opioid receptor kappa antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 100 nM1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID132269The compound was evaluated for antinociceptive potency using abdominal stretch assay in mice.1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID148693Opioid receptor kappa 1 antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 100 nM1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID234369Selectivity ratio (mu opioid receptors vs. delta opioid receptors).2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
AID148662Opioid receptor delta 1 antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at a concentration of 100 nM1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID309548Antinociceptive effect in mouse at 30 mg/kg by morphine assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID149937Opioid receptor delta 1 binding affinity was determined by inhibition of binding of [3H]DADLE to rat brain membrane2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
AID149544Binding affinity at kappa opioid receptor 1 in guinea pig brain by [3H]U-69593 displacement.2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
AID309544Selectivity for delta opioid receptor over mu opioid receptor2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID147987Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes.2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID148998Opioid receptor mu antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 100 nM1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID148835Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor kappa 11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID149279Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of Opioid receptor kappa 11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID147978Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of opioid receptor kappa1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID148040Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of Opioid receptor mu 11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID151151Binding affinity against Opioid receptor mu 1 using [3H][D-Ala2, MePhe4, Gly-ol5]-enkephalin as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
AID149074Binding affinity against Opioid receptor delta 1 using [3H][D-Ala2, D-Leu5]-enkephalin as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
AID309546Antinociceptive effect in mouse at 30 mg/kg by hot plate assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID76531Antagonistic activity against EK in guinea pig ileal longitudinal muscle (GPI)1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID76532Antagonistic activity against morphine in guinea pig ileal longitudinal muscle (GPI)1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID150043The compound was evaluated for binding affinity against Opioid receptor delta 1 in guinea pig brain membrane using [3H]- DPDPE as ligand1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID149011Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of opioid receptor mu1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID309542Displacement of [3H]p-Cl-DPDPE from delta opioid receptor2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID147839Selectivity for kappa to delta opioid receptors was determined1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID395145Binding affinity to delta opioid receptor in rat brain membrane2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
AID148810Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for opioid receptor delta 11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID309541Displacement of [3H]DAMGO from mu opioid receptor2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID148102The compound was evaluated for binding affinity against the opioid receptor kappa in guinea pig brain membranes using [3H]- U-69,5931992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID395146Ratio of Ki for kappa opioid receptor in rat brain membrane to Ki for mu opioid receptor in rat brain membrane2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
AID309543Displacement of [3H]U-69593 from cloned kappa opioid receptor2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID149907Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of Opioid receptor delta 11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID132874Antagonistic activity against morphine in smooth muscle preparation (MVD)1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID233862Selectivity between mu opioid receptor and delta opioid receptor.2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID233684Selectivity ratio of the affinity for kappa and delta opioid receptors (Ki mu/Ki delta)1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
AID148317Binding affinity against Opioid receptor kappa 1 using [3H]-U-69,593 as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
AID395144Binding affinity to kappa opioid receptor in rat brain membrane2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
AID78079The compound was tested for opioid agonist activity against guinea pig ileal longitudinal muscle (GPI)1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID310939Displacement of [3H]naltrindole from rat delta opioid receptor expressed in C6 cells2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity.
AID149206Opioid receptor delta antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at a concentration of 100 nM1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID149192Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of opioid receptor delta1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID233860Selectivity between kappa opioid receptor and delta opioid receptor.2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID150010Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor mu 11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID149023Selectivity for mu to delta opioid receptors was determined1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID149075Displacement of [3H]DADLE at delta-opioid receptor2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
AID309547Antinociceptive effect in mouse at 30 mg/kg by antiwrithing assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID395147Ratio of Ki for delta opioid receptor in rat brain membrane to Ki for mu opioid receptor in rat brain membrane2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
AID149872Opioid receptor mu 1 antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 100 nM1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID149020The compound was evaluated for binding affinity against opioid receptor mu in guinea pig brain membranes using [3H]- DAMGO as ligand1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID133921The compound was tested for opioid agonist activity against mouse vas deferens (MVD)1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID150841Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes.2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID151896Binding affinity at mu opioid receptor 1 in rat brain membrane by [3H]DAMGO displacement.2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
AID132873Antagonistic activity against DADLE in smooth muscle preparation (MVD)1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
AID233685Selectivity ratio of the affinity for mu and delta opioid receptors (Ki mu/Ki delta)1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
AID395143Binding affinity to mu opioid receptor in rat brain membrane2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
AID309545Antinociceptive effect in mouse at 30 mg/kg by tail flick assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
5'-halogenated analogs of oxymorphindole.
AID235355Selectivity ratio (Ki value towards mu receptor compared to that of delta receptor).2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (38.89)18.2507
2000's9 (50.00)29.6817
2010's2 (11.11)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: 11.30

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

MetricThis Compound (vs All)
Research Demand Index11.30 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.30 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (94.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]