Page last updated: 2024-12-11

enkephalin, leucine-2-alanine

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Description

Enkephalin, Leucine-2-Alanine: A delta-selective opioid (ANALGESICS, OPIOID). It can cause transient depression of mean arterial blood pressure and heart rate. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6917707
CHEMBL ID340032
SCHEMBL ID11124725
MeSH IDM0024921

Synonyms (36)

Synonym
gtpl1607
[d-ala2, d-leu5]-enkephalin
dadle
bw-180c
dadl
enkephalin-leu,ala(2)
(d-ala2,d-leu5)enkephalin
d-leucine, n-(n-(n-(n-l-tyrosyl-d-alanyl)glycyl)-l-phenylalanyl)-
2-alanyl-leucine enkephalin
leucine enkephalin-2-alanine
enkephalin, leucine-2-alanine
5-leucine-2-alanine enkephalin
chembl340032 ,
[d-ala2-d-leu5]enkephalin
bdbm21025
dadle-oh
(d-ala2,d-leu5)-enkephalin
(2r)-2-[(2s)-2-{2-[(2r)-2-[(2s)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanamido]-4-methylpentanoic acid
h-tyr-d-ala-gly-phe-d-leu-oh
63631-40-3
(2r)-2-[[(2s)-2-[[2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid
hb4qd9gl6f ,
unii-hb4qd9gl6f
SCHEMBL11124725
AKOS024457800
HY-105343
CS-0025794
h-tyr-d-ala-gly-phe-d-leu
Q424905
DB08856
l-tyrosyl-d-alanylglycyl-l-phenylalanyl-d-leucine
enkephalin-(2-d-ala, 5-d-leu)
tyr-d-ala-gly-phe-d-leu
tyrosyl-d-alanylglycylphenylalanyl-d-leucine
d-leucine, l-tyrosyl-d-alanylglycyl-l-phenylalanyl-
(d-ala2-d-leu5)enkephalin

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"In vitro stability and in vivo pharmacokinetic studies of a model opioid peptide, H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE), and its cyclic prodrugs (acyloxyalkoxy-based cyclic prodrug of DADLE, coumarinic acid-based cyclic prodrug of DADLE, and oxymethyl-modified coumarinic acid-based cyclic prodrug of DADLE) were conducted."( In vitro stability and in vivo pharmacokinetic studies of a model opioid peptide, H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE), and its cyclic prodrugs.
Borchardt, RT; Chen, W; Yang, JZ, 2002
)
0.31

Bioavailability

ExcerptReferenceRelevance
" Bioavailability was estimated following intramuscular (i/m) and intranasal (i/n) routes of administration of 3H-dalargin in anesthetized dogs."( [Bioavailability of dalargin and its metabolism during intranasal administration to rats].
Kalenikova, EI; Sokolov, AS; Vinogradov, VA, 1988
)
0.27
" Studies have proven the brain uptake of Tween 80 overcoated nanoparticles after intravenous administration, but studies for brain delivery of nanoparticles after oral administration had been limited due to reduced bioavailability of nanoparticles and extensive degradation of the peptide and/or nanoparticles by gastrointestinal enzymes."( Double-coated poly (butylcynanoacrylate) nanoparticulate delivery systems for brain targeting of dalargin via oral administration.
Das, D; Lin, S, 2005
)
0.33

Dosage Studied

ExcerptRelevanceReference
" 1) In the presence of a fixed dose of DPDPE (150 nmol), there was a left shift in the dose-response curve of the mu agonist, with the magnitude of the shifts being greater than those anticipated from a simple additive interaction: PL017 (31-fold) > or = DAMGO (20-fold) > morphine (6."( Isobolographic and dose-response analyses of the interaction between intrathecal mu and delta agonists: effects of naltrindole and its benzofuran analog (NTB).
Malmberg, AB; Yaksh, TL, 1992
)
0.28
" On day 7, the magnitude of tolerance was assessed by establishing dose-response curves for the effect of the chronic drug given as an intrathecal bolus."( Studies of morphine and D-ala2-D-leu5-enkephalin (DADLE) cross-tolerance after continuous intrathecal infusion in the rat.
Stevens, CW; Yaksh, TL, 1992
)
0.28
" To test for a specific toxic effect on the neurons of the ciliary ganglion, we generated a dose-response curve for toxicity in vitro and determined that naltrexone was not toxic over concentration ranges that are likely to exist in vivo."( Endogenous opioids modulate neuronal survival in the developing avian ciliary ganglion.
Ford, MJ; Meriney, SD; Oliva, D; Pilar, G, 1991
)
0.28
"The effect of intravenous infusion of agonists of mu-(DAGO) and delta-(DADL, DAAE) opiate receptors on mean arterial pressure and heart rate was studied in experiments on rats with dosed blood loss of up to 30% of calculated blood volume."( [The effect of opiate receptor agonists on the blood circulation in rats with hemorrhagic shock].
Grossler, Iu; Sheĭkh, DV; Slepushkin, VD,
)
0.13
" The depressive effects induced by the mu agonist PL017 (5 micrograms), delta agonist DADLE (25 micrograms) and kappa agonist 66A-078 (1 microgram) were antagonized by CCK-8 within a dosage of 10 micrograms in a dose dependent manner."( [Cholecystokinin-octapeptide antagonizes the central depressive effect of opioid peptides in rats].
Han, JS; Mei, L, 1991
)
0.28
" The FHR response to DADLE was similar to DAGO in both dose-response and time-action characteristics."( Central opioid modulation of fetal cardiovascular function: role of mu- and delta-receptors.
Cai, LQ; Szeto, HH; Zhu, YS, 1990
)
0.28
") injected 1 min before each agonist produced a significant parallel shift to the right of the dose-response curves for morphine and DAMGO, but only partly antagonized the effects of DADLE and DSLET."( Role of peripheral mu, delta and kappa opioid receptors in opioid-induced inhibition of gastrointestinal transit in rats.
La Regina, A; Petrillo, P; Sbacchi, M; Tavani, A, 1990
)
0.28
" Dose-response curves at 1 hr revealed similar potencies of oxymorphone and the derivatives, with the exception of OxyPNPH which was significantly less potent."( Irreversible opiate agonists and antagonists. IV. Analgesic actions of 14-hydroxydihydromorphinone hydrazones.
Bodnar, RJ; Burks, TF; Clark, JE; Hahn, EF; Pasternak, GW; Williams, CL, 1988
)
0.27
" dose-response curves for the effect of the chronic drug given as a bolus."( Potency of infused spinal antinociceptive agents is inversely related to magnitude of tolerance after continuous infusion.
Stevens, CW; Yaksh, TL, 1989
)
0.28
" However, in mice tested with the naltrexone pellets still implanted, the 15 mg naltrexone pellet was able to shift the dose-response function for morphine analgesia more than 300-fold."( Chronic opioid antagonist treatment: assessment of receptor upregulation.
Lutfy, K; Sierra, V; Yoburn, BC, 1989
)
0.28
" The dose-response curves were monotonic and the slopes were log-linear."( Epidural injections of bupivacaine, morphine, fentanyl, lofentanil, and DADL in chronically implanted rats: a pharmacologic and pathologic study.
Durant, PA; Yaksh, TL, 1986
)
0.27
" Naloxonazine (10 mg/kg) shifted the morphine hyperphagia dose-response curve to the right."( Differential sensitivity of opioid-induced feeding to naloxone and naloxonazine.
Arjune, D; Bodnar, RJ; Hahn, EF; Mann, PE; Pasternak, GW; Romero, MT, 1988
)
0.27
" Full dose-response curves show a 4-fold shift to the right (P less than ."( Separation of opioid analgesia from respiratory depression: evidence for different receptor mechanisms.
Ling, GS; Lockhart, SH; Pasternak, GW; Spiegel, K, 1985
)
0.27
" The dose-response curves for the biological response were suggestive of positive cooperativity and systematically occurred at lower ligand concentrations than those for the binding of [3H] [D-Ala2, D-Leu5]enkephalin (DADLE), which were instead shallow and suggestive of a site heterogeneity or of a cooperative phenomenon."( Multiple states of opioid receptors may modulate adenylate cyclase in intact neuroblastoma X glioma hybrid cells.
Costa, T; Gramsch, C; Herz, A; Wüster, M, 1985
)
0.27
" The slope of the analgesic dose-response curve for the highly specific delta agonist, cyclic [D-Penicillamine2, D-Penicillamine5]enkephalin (DPDPE), was significantly different (flatter) from those of mu agonists or DADLE."( Continuous intrathecal opioid analgesia: tolerance and cross-tolerance of mu and delta spinal opioid receptors.
Chang, KJ; Leslie, JB; Russell, RD; Su, YF; Watkins, WD, 1987
)
0.27
"The effects of the delta-selective antagonist ICI 174864 and naltrexone on the dose-response curves to the mu-selective agonist RX 783006 and D-ala-D-leucine enkephalin (DADL) have been investigated in the rat isolated vas deferens preparation (RVD) set up in Krebs solution containing half the normal Ca++ concentration."( Delta receptors in the rat vas deferens.
Carter, A; Smith, CF, 1986
)
0.27
" The dose-response function was U-shaped, with neither 100 nor 600 micrograms/kg having any effect."( Leu-enkephalin impairs memory of an appetitive maze response in mice.
Linden, D; Martinez, JL, 1986
)
0.27
" A similar effect was obtained only with a dose 25 times higher (500 ng X kg-1) administered intravenously; at this dosage DALAMIDE administered intravenously also reduced the colonic motility index by 66%."( Central and peripheral control of gastrointestinal and colonic motility by endogenous opiates in conscious dogs.
Bueno, L; Fargeas, MJ; Fioramonti, J; Hondé, C; Primi, MP, 1985
)
0.27
") produced a dose-response curve with a reduced maximum effect."( Relative involvement of receptor subtypes in opioid-induced inhibition of intestinal motility in mice.
Takemori, AE; Ward, SJ,
)
0.13
") shifted the dose-response curve for both responses to the right more for the beta-EP than for DADL."( Inhibition of tail-flick and shaking responses by intrathecal and intraventricular D-Ala2-D-Leu5-enkephalin and beta-endorphin in anesthetized rats.
Cheng, SS; Fujimoto, JM; Tseng, LF, 1983
)
0.27
" Uptake of [3H]DADLE was a receptor-mediated process, since it was inhibited by opiate receptor ligands and the (i) time course, (ii) dose-response curve, and (iii) temperature dependence of uptake were similar to those for enkephalin-receptor down regulation."( Characterization of the association of tritiated enkephalin with neuroblastoma cells under conditions optimal for receptor down regulation.
Blanchard, SG; Chang, KJ; Cuatrecasas, P, 1983
)
0.27
" It increased the IC50 values and slopes of their dose-response curve for enkephalins and their analogs, and shifted to the right the curves for FK33824, levorphanol and normorphine."( Functional opiate receptor in mouse vas deferens: evidence for a complex interaction.
Garzón, J; Lee, NM; Sánchez-Blázquez, P, 1983
)
0.27
" In conscious man essentially similar results were found following intravenous dosing with a stable met-enkephalin analogue (DAMME, FK33824) or naloxone with decreases and increases respectively in the sensitivity of baroreflex responses to sodium nitroprusside."( Opioid peptides and central control of blood pressure.
Petty, MA; Reid, JL; Rubin, PC, 1984
)
0.27
" Respiratory frequency was dose-dependently depressed by FK-33824 and DADLE ; dose-response curves with morphine and D-Ser2- Thr6 could not be obtained for technical reasons."( A comparative study in rats of the respiratory depression and analgesia induced by mu- and delta-opioid agonists.
Flórez, J; Pazos, A, 1984
)
0.27
", delayed nociceptive reaction on a 55 degrees C hot-plate with a dose-response curve not readily fitting a single straight line; this effect was antagonized by high doses of naloxone."( Bremazocine induces antinociception, but prevents opioid-induced constipation and catatonia in rats and precipitates withdrawal in morphine-dependent rats.
Gambino, MC; Petrillo, P; Tavani, A, 1984
)
0.27
" Finally dose-response curves were found highly reproducible across transfection experiments, opening the possibility for a direct comparison of distinct recombinant receptor preparations."( [35S]GTP gamma S binding: a tool to evaluate functional activity of a cloned opioid receptor transiently expressed in COS cells.
Befort, K; Kieffer, BL; Tabbara, L, 1996
)
0.29
" Locomotor activity dramatically decreased in mice dosed with PBCA NP, but not with PS NP."( Indirect evidence that drug brain targeting using polysorbate 80-coated polybutylcyanoacrylate nanoparticles is related to toxicity.
Cecchelli, R; Chauvet, R; Couet, W; Fenart, L; Olivier, JC; Pariat, C, 1999
)
0.3
" However, the dose-response curves of the protective effects of DADLE are U-shaped as judged by three biochemical or morphological assays: the LDH release, the DNA laddering, and the apoptotic nuclei."( Antiapoptotic and cytotoxic properties of delta opioid peptide [D-Ala(2),D-Leu(5)]enkephalin in PC12 cells.
Hayashi, T; Su, TP; Tsao, LI, 2002
)
0.31
"Previously, our laboratory reported that cyclic peptide prodrugs of the opioid peptide H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE) are metabolized by cytochrome P450 (CYP450) enzymes, which limits their systemic exposure after oral dosing to animals."( Factors that restrict the cell permeation of cyclic prodrugs of an opioid peptide, part 3: Synthesis of analogs designed to have improved stability to oxidative metabolism.
Borchardt, RT; Fuchs-Knotts, T; Nofsinger, R, 2012
)
0.38
" However, the relative dose-response effects of DADLE still remain unclear."( Dose-dependent neuroprotection of delta-opioid peptide [D-Ala(2), D-Leu(5)] enkephalin on spinal cord ischemia-reperfusion injury by regional perfusion into the abdominal aorta in rabbits.
Chen, B; Li, S; Liu, H; Yao, J, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-P receptorRattus norvegicus (Norway rat)Ki0.00810.00070.12981.0000AID1798029
Substance-P receptorCavia porcellus (domestic guinea pig)Ki0.00130.00130.69133.4000AID288852
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.09150.00010.729810.0000AID145926; AID148653; AID148661
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00170.00030.38877.0000AID149505; AID149520
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00030.00000.60689.2330AID149804
Kappa-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.00900.00131.538010.0000AID145926
Mu-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.04190.00010.887410.0000AID151303
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00950.00000.38458.6000AID151758; AID1798029; AID288853
Delta-type opioid receptorHomo sapiens (human)Ki0.00590.00000.59789.9300AID1798029; AID288852
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)1.46910.00030.71237.0700AID148565; AID148681
Mu-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.00900.00081.699210.0000AID145926
[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 receptorRattus norvegicus (Norway rat)Kd7.50050.00212.598510.0000AID149052; AID149533
Mu-type opioid receptorRattus norvegicus (Norway rat)Kd6.00460.00021.296510.0000AID149052; AID151464; AID152211
Kappa-type opioid receptorRattus norvegicus (Norway rat)Kd7.65620.00001.806910.0000AID148456; AID149052
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.93640.00000.32639.4000AID1129817; AID1543763; AID1543764
Mu-type opioid receptorHomo sapiens (human)Kd0.62500.00010.18250.8300AID148456
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)0.47810.00000.43328.3000AID1129820; AID1543765; AID1685504
Delta-type opioid receptorHomo sapiens (human)Kd0.62500.00040.51471.9800AID148456
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Kd0.00210.00211.44444.8940AID149533
Kappa-type opioid receptorHomo sapiens (human)Kd0.62500.00000.06700.8300AID148456
Mu-type opioid receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.05400.00000.04930.9320AID1129820
[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 (91)

Assay IDTitleYearJournalArticle
AID151303Inhibition of [3H]- DAMGO binding to Rat brain Opioid receptor mu 11996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID149050Inhibition of [3H]naloxone receptor binding to opioid receptor in the presence of 100 mM NaCl1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID1685506Activity at human MOR expressed in CHOK1 cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment measured after 90 mins by PathHunter assay2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID288860Agonist activity at mu opioid receptor in Hartley guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID1543765Agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in DOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay2019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID149505Inhibition of [3H]- DADLE binding to Rat brain Opioid receptor delta 11996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID149871The opioid activity against the mu-receptor in the isolated guinea pig ileum(GPI)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
AID1543772Potency index, ratio of test compounds intrinsic activity to DADLE intrinsic activity for agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta12019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1543764Agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to MOR/beta-arrestin-2 assessed as increase in MOR/beta-arrestin-2 protein interaction incubated for 5 mins in presence of coelenterazi2019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1129817Agonist activity at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
AID1685502Agonist activity at human KOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID149864Inhibitory potency against Opioid receptor mu 1 in longitudinal muscle preparation of guinea pig ileum1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
AID123808Relative potency of compound verses morphine for analgesic activity in mice1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
AID149804Binding affinity against Opioid receptor delta 1 in P2 membrane preparation of rat brain by [3H]DADLE displacement.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Function of negative charge in the "address domain" of deltorphins.
AID1685505Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay relative to DAMGO2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID73710Displacement of specifically bound [3H]naloxone from guinea pig ileum, in the presence of 100 mM NaCl1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
Novel analogues of enkephalin: indentification of functional groups required for biological activity.
AID148671Antagonist activity of against Opioid receptor delta 1 from Mouse vas deferens preparation at the concentration of 500 nm1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Naltrindole 5'-isothiocyanate: a nonequilibrium, highly selective delta opioid receptor antagonist.
AID123332Analgesic activity of compound in mice after icv administration1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
AID1543766Agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-2 assessed as increase in DOR/beta-arrestin-2 protein interaction incubated for 5 mins in presence of coelenterazine b2019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1129821Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes after 1 hr2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
AID1685508Bias factor, ratio of biased agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin2 EFC recruitment to biased agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as inhibi2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID148565Inhibition of [3H]- U69,593 binding to Guinea pig Opioid receptor kappa 11996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID228347Ratio of Ki values for mu and delta opioid receptors.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Function of negative charge in the "address domain" of deltorphins.
AID129183Analgesic activity in mice by tail-flick test after intracerebroventricular administration at a dose of 240 ug/mouse after time duration of 2 minutes; no of mice survived / total no of mice tested-61984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Replacement of the peptide-backbone amides connecting Tyr-Gly and Gly-Gly in leucine-enkephalin with ketomethylene groups: synthesis and biological activity.
AID77991Inhibition of contraction of electrically stimulated guinea pig ileum1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
Novel analogues of enkephalin: indentification of functional groups required for biological activity.
AID175509Displacement of specifically bound [3H]naloxone from rat brain homogenate, in the absence of NaCl1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
Novel analogues of enkephalin: indentification of functional groups required for biological activity.
AID234731Selectivity as the ratio of IC50 value against mu receptor (GPI) to that of delta receptor (MVD).1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
AID1543773Potency index, ratio of test compounds intrinsic activity to DADLE intrinsic activity for agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-22019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1685501Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay relative to DAMGO2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID615024Half life in human plasma2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
QSAR models for predicting enzymatic hydrolysis of new chemical entities in 'soft-drug' design.
AID148653Inhibitory potency against delta Opioid receptor delta 1 in longitudinal muscle preparation of mouse vas deferens1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
AID148661Opioid activity against delta-receptor of isolated mouse vas deferens(MVD) at 30 uM1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
AID288861Ratio of IC50 for mu opioid receptor in GPI assay to IC50 for delta opioid receptor in MVD assay2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID149730Agonistic activity for Opioid receptor mu 1 as inhibitory activity towards electrically stimulated guinea pig ileum1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID1129809Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
AID1543770Potency index, ratio of test compounds EC50 to DADLE EC50 for agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta12019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID288853Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID148456Compound was evaluated for Opioid receptor kappa 1 affinity against the receptor site model site 4(kappa)1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID1685507Activity at human MOR expressed in CHOK1 cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment measured after 90 mins by PathHunter assay relative to control2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID229309Ratio of IC50 compared to [D-Ala2, D-Leu5]-enkephalin in guinea pig ileum assay1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
Novel analogues of enkephalin: indentification of functional groups required for biological activity.
AID150409The compound was evaluated for opioid receptors binding affinity competition with [3H]diprenorphine. 1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Brain-targeted delivery of a leucine-enkephalin analogue by retrometabolic design.
AID149533Affinity against the Opioid receptor delta 11986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID1543779Selectivity ratio of agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in MOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazi2019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1543776Bias factor, change in deltalog(Tau/KA) for agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in MOR/G beta1 protein interaction incubated for 5 mins in p2019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1685500Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID148892Compound was tested for antagonistic activity against opioid receptor in mouse vas deferens1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors.
AID1543763Agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in MOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay2019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID149048Inhibition of [3H]naloxone receptor binding to opioid receptor in the absence of 100 mM NaCl1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID152060Ability to inhibit the binding of [3H]-DAGO to Opioid receptor mu 1 in rat brain membranes1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
AID151464Opioid receptor mu 1 affinity against the receptor site model site 1 (mu1)1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID125747Analgesic potency in mice after icv injection and 10 min before exposing to hot plate1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
AID1543767Potency index, ratio of test compounds EC50 to DADLE EC50 for agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta12019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID680763TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.004 uM, DADLE: 1000 uM) in Xenopus laevis oocytes2003The Journal of pharmacy and pharmacology, Jul, Volume: 55, Issue:7
Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin.
AID56303Agonistic activity towards Opioid receptor delta 1 as inhibitory activity towards electrically stimulated mouse vas deferens1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID288852Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID151758Binding affinity against Opioid receptor mu 1 in P2 membrane preparation of rat brain by [3H]DAGO displacement.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Function of negative charge in the "address domain" of deltorphins.
AID233531The ratio between [3H]naloxone binding in the presence and absence of 100 mM NaCl1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID229954Relative affinity mu and delta opioid receptors of rat brain1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID139638Antagonist activity in mouse vas deferens preparation.1984Journal of medicinal chemistry, Oct, Volume: 27, Issue:10
Activities of morphinone and N-(cyclopropylmethyl)normorphinone at opioid receptors.
AID152211Opioid receptor mu 2 affinity against the receptor site model site 2(mu2)1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID1129820Agonist activity at GFP-fused delta opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
AID1129819Intrinsic efficacy at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay relative to untreated control2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
AID229261Ratio of IC50 evaluated in GPI to MVD1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
AID1685509Activity at human MOR expressed in U2OS cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment by Tango assay2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID1685510Activity at human MOR expressed in U2OS cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment by Tango assay relative to control2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID151439Inhibition of [3H]DADLE radioligand binding to rat brain delta-opioid receptor; not determined1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
AID145926Concentration required to inhibit the specific binding of tritiated ligand [3H]DADL to opiate receptor by 50%1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Replacement of the peptide-backbone amides connecting Tyr-Gly and Gly-Gly in leucine-enkephalin with ketomethylene groups: synthesis and biological activity.
AID1685504Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID288859Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
AID132843Irreversible antagonistic potency in mouse vas deferens (MVD)1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Importance of C-6 chirality in conferring irreversible opioid antagonism to naltrexone-derived affinity labels.
AID1129808Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
AID149520Inhibition of [3H]DADLE radioligand binding to rat brain opioid receptor delta 1.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
AID1543768Potency index, ratio of test compounds EC50 to DADLE EC50 for agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-22019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID148681Inhibition of [3H]-U-69,593 radioligand binding to Guinea pig Opioid receptor kappa 1; not determined1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
AID149646Inhibition of [3H]DSLET binding to delta 1 opioid receptors in rat brain membranes1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
AID1685503Agonist activity at human KOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay relative to DAMGO2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID1129822Displacement of [3H]DPDPE from delta opioid receptor in guinea pig brain membranes after 1 hr2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
AID149052Compound was evaluated for opioid receptor affinity against the receptor site model site 51986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID1543771Potency index, ratio of test compounds EC50 to DADLE EC50 for agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-22019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1543775Potency index, ratio of test compounds intrinsic activity to DADLE intrinsic activity for agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-22019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID232381Relative EC50 compared to [D-Ala2, D-Leu5]-enkephalin without NaCl in rat brain assay1980Journal of medicinal chemistry, Oct, Volume: 23, Issue:10
Novel analogues of enkephalin: indentification of functional groups required for biological activity.
AID1543774Potency index, ratio of test compounds intrinsic activity to DADLE intrinsic activity for agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta12019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1543769Bias factor, change in deltalog(Tau/KA) for agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in DOR/G beta1 protein interaction incubated for 5 mins in p2019European journal of medicinal chemistry, Apr-15, Volume: 168(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
AID1685511Bias factor, ratio of biased agonist activity at human mu opiod receptor expressed in U2OS cells assessed as stimulation of beta-arrestin2 EFC recruitment to biased agonist activity at human mu opiod receptor expressed in U2OS cells assessed as inhibition2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
G-Protein biased opioid agonists: 3-hydroxy-
AID229952Relative affinity for rat brain kappa1 and guinea pig delta opioid receptors1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID148670Antagonist activity of against Opioid receptor delta 1 from Mouse vas deferens preparation at the concentration of 100 nm1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Naltrindole 5'-isothiocyanate: a nonequilibrium, highly selective delta opioid receptor antagonist.
AID229953Relative affinity for mouse vas deferens (mu receptor) and guinea pig ileum (delta receptor)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
AID1346373Mouse delta receptor (Opioid receptors)1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
AID1346364Human mu receptor (Opioid receptors)1998NIDA research monograph, Mar, Volume: 178Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1346361Human delta receptor (Opioid receptors)1998NIDA research monograph, Mar, Volume: 178Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1798029Radioligand Labeled Binding Assay from Article 10.1021/jm061369n: \\Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.\\2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,408)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990692 (49.15)18.7374
1990's471 (33.45)18.2507
2000's164 (11.65)29.6817
2010's73 (5.18)24.3611
2020's8 (0.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 6.79

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 Index6.79 (24.57)
Research Supply Index7.38 (2.92)
Research Growth Index4.17 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (6.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials23 (1.45%)5.53%
Reviews20 (1.27%)6.00%
Case Studies6 (0.38%)4.05%
Observational0 (0.00%)0.25%
Other1,532 (96.90%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]