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ici 174865

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Description

ICI 174865: delta opioid receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44149909
CHEMBL ID47545
MeSH IDM0244963

Synonyms (23)

Synonym
CHEMBL47545 ,
2-[2-(2-{2-[2-diallylamino-3-(4-hydroxy-phenyl)-propionylamino]-2-methyl-propionylamino}-2-methyl-propionylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid
bdbm50006946
ici-174865
92535-15-4
n,n-diallyl-tyrosyl-aminoisobutyryl-aminoisobutyryl-phenylalanyl-leucine
n-(n-(n-(n-(n,n-di-2-propenyl-l-tyrosyl)-2-methylalanyl)-2-methylalanyl)-l-phenylalanyl)-l-leucine
ici 174865
ici 174,865
l-leucine, n-(n-(n-(n-(n,n-di-2-propenyl-l-tyrosyl)-2-methylalanyl)-2-methylalanyl)-l-phenylalanyl)-
ici-174,865
n,n-diallyl-tyr-aib-aib-phe-leu-oh
ici 174,864
n,n-diallyl-tyr-aib-aib-phe-leu
AKOS024458657
Y-100013
l-leucine,n,n-di-2-propen-1-yl-l-tyrosyl-2-methylalanyl-l-phenylalanyl-
(2s,5s,14s)-15-allyl-5-benzyl-14-(4-hydroxybenzyl)-2-isobutyl-8,8,11,11-tetramethyl-4,7,10,13-tetraoxo-3,6,9,12,15-pentaazaoctadec-17-en-1-oic acid
n-{2-benzyl-1,4,7,10-tetrahydroxy-11-[(4-hydroxyphenyl)methyl]-5,5,8,8-tetramethyl-12-(prop-2-en-1-yl)-3,6,9,12-tetraazapentadeca-3,6,9,14-tetraen-1-ylidene}leucine
DTXSID10919119
nih10893
PD071343
l-leucine, n,n-di-2-propen-1-yl-l-tyrosyl-2-methylalanyl-2-methylalanyl-l-phenylalanyl-
[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)
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.70300.00010.729810.0000AID148523
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)18.90000.00030.38877.0000AID151284
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)0.08300.00020.75218.0140AID270160
Delta-type opioid receptorHomo sapiens (human)Ki0.01910.00000.59789.9300AID148237
[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)
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)0.11600.00000.43328.3000AID1237282
[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)Ke0.06900.00010.14726.1080AID148810; AID148930
Delta-type opioid receptorRattus norvegicus (Norway rat)Activity0.03700.00000.11931.2200AID310939
Mu-type opioid receptorHomo sapiens (human)Ke0.04200.00000.24883.0700AID150831; AID270152
Delta-type opioid receptorHomo sapiens (human)Ke0.00790.00010.69799.0700AID148098; AID270153
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ke0.83590.00000.03891.1570AID148098; AID148835
Kappa-type opioid receptorHomo sapiens (human)Ke0.33900.00000.35405.8100AID147876; AID270154
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ke1.66700.00000.01590.0430AID150010
[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
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (70)

Assay IDTitleYearJournalArticle
AID130271Ratio of IC50 of morphine (agonist) expossed to the compound for 10 min and then washed 30 times to Ratio of IC50 of morphine (agonist) prior to exposure to compound1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
AID270158Intrinsic activity at mu opioid receptor in presence of 1 uM GDP2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID232963Ke selectivity ratio (mu/delta) of the compound1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID270160Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID270161Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP relative to control2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID148775Reversible opioid agonist activity in the electrically stimulated mouse vas deferens(MVD) at 1 uM concentration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
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.
AID270157Agonist activity at delta opioid receptor at 31.6 uM2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID148488Reversible opioid agonist activity in the electrically stimulated guinea pig ileum(GPI) at 1 uM concentration (Exp 1)1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
AID232962Ke selectivity ratio (kappa/delta) of the compound1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID148237Binding affinity towards opioid receptor delta 1 expressed in CHO cells was determined by using [3H]DPDPE as radioligand2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
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.
AID148815Ratio of IC50 of ethylketazocine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor kappa 1 at 1 uM in GPI assay1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
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.
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.
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.
AID150831Ability to inhibit agonist-stimulated (DAMGO) [35S]GTP-gamma-S, binding, using cloned human Opioid receptor mu 1
expressed in CHO cells
2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
AID147876Ability to inhibit agonist-stimulated (U69,593) [35S]GTP-gamma-S, binding, using cloned human Opioid receptor kappa 1 expressed in CHO cells2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
AID148788Ratio of IC50 of DADLE (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in the absence of compound for Opioid receptor delta 1 at 10 uM in MVD assay1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
AID233951Ratio of IC50 against mu opioid receptor to that of delta opioid receptor2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
AID1237283Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay relative to control2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists.
AID232965Ki selectivity ratio (mu/delta) of the compound1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID270159Intrinsic activity at kappa opioid receptor in presence of 1 uM GDP2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID148254Evaluation for the ability of kappa opioid to protect the [3H]-DAMGO binding site from alkylation1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties.
AID149881Ratio of IC50 of morpholine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor mu 1 at 1 uM in GPI assay1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
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.
AID148930Compound was evaluated for antagonist potency in the mouse vas deferens preparation using [D-Ala2,D-Leu5]enkephalin (Opioid receptor delta 1)1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID151141Ratio of IC50 of morpholine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor mu 1 at 1 uM in MVD assay1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
AID130268Ratio of IC50 of DADLE (agonist) expossed to the compound for 10 min and then washed 30 times to Ratio of IC50 of morphine (agonist) prior to exposure to compound1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
AID233662Selectivity ratio of agonist stimulated [35S]GTP-gamma-S, binding in cloned human kappa-opioid receptor versus delta-opioid receptor2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
AID148523Binding affinity was measured in cloned Opioid receptor delta 1 expressed in CHO cells using [3H]- DPDPE as radioligand.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
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.
AID149367Evaluation for the ability of delta opioid to protect the [3H]-DAMGO binding site from alkylation1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties.
AID149283Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID148098Ability to inhibit agonist-stimulated (DPDPE) [35S]GTP-gamma-S, binding, using cloned human opioid receptor delta 1 expressed in CHO cells2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
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.
AID151284Binding affinity was measured in cloned Opioid receptor mu 1 expressed in CHO cells using [3H]- DAMGO as radioligand.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
AID151142Ratio of IC50 of morpholine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor mu 1 at 10 uM in GPI assay1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
AID233663Selectivity ratio of agonist stimulated [35S]GTP-gamma-S, binding in cloned human mu-opioid receptor versus delta-opioid receptor2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
AID270155Selectivity for human cloned delta opioid receptor over mu opioid receptor2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID148489Reversible opioid agonist activity in the electrically stimulated guinea pig ileum(GPI) at 1 uM concentration (Exp 2)1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
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.
AID138825Evaluation for the ability of mu opioid to protect the [3H]DAMGO binding site from alkylation1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties.
AID270153Antagonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 10 uM GDP2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID270156Selectivity for human cloned delta opioid receptor over kappa opioid receptor2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
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.
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.
AID149910Compound was evaluated for binding affinity at Opioid receptor delta 1 in guinea pig brain membranes1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID148961Compound was evaluated for antagonist potency in guinea pig ileum preparation using ethylketazocine (Opioid receptor kappa 1)1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID148787Ratio of IC50 of DADLE (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in the absence of compound for Opioid receptor delta 1 at 1 uM in MVD assay1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
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.
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.
AID232964Ki selectivity ratio (kappa/delta) of the compound1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID270154Antagonist activity at human cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of U69593-stimulated [35S]GTPgammaS binding in presence of 10 uM GDP2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID270152Antagonist activity at human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTP-gamma-S binding in presence of 10 uM GDP2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
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.
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.
AID150029Compound was evaluated for antagonist potency in guinea pig ileum preparation using morphine (Opioid receptor mu 1)1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
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.
AID148774Reversible opioid agonist activity in the electrically stimulated mouse vas deferens(MVD) at 10 uM of concentration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor.
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.
AID233705Selectivity ratio was determined from Ke value of Opioid receptor kappa 1 and Opioid receptor delta 11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
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.
AID148041Compound was evaluated for binding affinity at Opioid receptor mu 1 in guinea pig brain membranes1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID233878Selectivity ratio was determined from Ke value of Opioid receptor mu 1 and Opioid receptor delta 11990Journal 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.
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.
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.
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.
AID1237282Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (8.33)18.7374
1990's5 (41.67)18.2507
2000's5 (41.67)29.6817
2010's1 (8.33)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: 12.43

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 Index12.43 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index5.07 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.43)

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%
Other13 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]