Page last updated: 2024-12-11

dermorphin

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Description

dermorphin: opiate-like peptide present in amphibian skin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5485199
CHEMBL ID278789
CHEBI ID177767
SCHEMBL ID237169
MeSH IDM0095400

Synonyms (29)

Synonym
77614-16-5
(2s)-n-[(2s)-1-amino-3-hydroxy-1-oxopropan-2-yl]-1-[(2s)-2-[[2-[[(2s)-2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carboxamide
CHEBI:177767
dermorphin
tyrosyl-alanyl-phenylalanyl-glycyl-tyrosyl-prolyl-serinamide
h-tyr-d-ala-phe-gly-tyr-pro-ser-nh2
CHEMBL278789 ,
yafgyps-nh2
1-[2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid (1-carbamoyl-2-hydroxy-ethyl)-amide
(s)-1-[(s)-2-[2-((s)-2-{(r)-2-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid ((s)-1-carbamoyl-2-hydroxy-ethyl)-amide
dermorphin;1-[2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid (1-carbamoyl-2-hydroxy-ethyl)-amide
tyr-ala-phe-gly-tyr-pro-ser
bdbm50059841
1-[2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid (1-carbamoyl-2-hydroxy-ethyl)-amide(dermorphin)
1-[2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid (1-carbamoyl-2-hydroxy-ethyl)-amide (dermorphin)
C20030
2sec01b703 ,
unii-2sec01b703
l-serinamide, l-tyrosyl-d-alanyl-l-phenylalanylglycyl-l-tyrosyl-l-prolyl-
tyr-d-ala-phe-gly-tyr-pro-ser-nh2
SCHEMBL237169
DTXSID40228281
HY-P0244
dermorphin acetate
EX-A7078
tyr-dala-phe-gly-tyr-pro-ser-nh2
(s)-n-((s)-1-amino-3-hydroxy-1-oxopropan-2-yl)-1-((2s,8s,11r,14s)-14-amino-8-benzyl-2-(4-hydroxybenzyl)-15-(4-hydroxyphenyl)-11-methyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecane)pyrrolidine-2-carboxamide
Q1771654
MS-31482

Research Excerpts

Overview

Dermorphin is a unique opioid peptide that is 30-40 times more potent than morphine. The Dermorphins are a family of peptides that act as potent agonists of the opioid μ receptor.

ExcerptReferenceRelevance
"Dermorphin is a peptide with analgesic actions similar to morphine, but with greater effect and less potential to cause tolerance. "( A high throughput approach for determination of dermorphin in human urine using liquid chromatography-mass spectrometry for doping control purposes.
Castro, JL; de Sousa, VP; Martucci, MEP; Pereira, HMG, 2020
)
2.26
"Dermorphin is a heptapeptide with an analgesic potential higher than morphine that does not present the same risk for the development of tolerance. "( Evaluation of Dermorphin Metabolism Using Zebrafish Water Tank Model and Human Liver Microsomes.
de L Castro, J; de Sousa, VP; Martucci, MEP; Pereira, HMG, 2021
)
2.42
"Dermorphin is a unique opioid peptide that is 30-40 times more potent than morphine. "( Detection, quantification, and identification of dermorphin in equine plasma and urine by LC-MS/MS for doping control.
Guan, F; Li, X; Maylin, GA; Robinson, M; Soma, LR; Uboh, CE, 2013
)
2.09
"The Dermorphins are a family of peptides that act as potent agonists of the opioid μ receptor. "( A high throughput screen for 17 Dermorphin peptides in equine and human urine and equine plasma.
Levina, V; Steel, R; Timms, M; Vine, J, 2014
)
1.24
"Dermorphin is a μ-opioid receptor-binding peptide that causes both central and peripheral effects following intravenous administration to rats, dogs, and humans and has been identified in postrace horse samples. "( Pharmacokinetics and pharmacodynamics of dermorphin in the horse.
Guan, F; McDonnell, S; Robinson, MA; Soma, LR; Uboh, CE, 2015
)
2.13
"Dermorphin is a heptapeptide (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH(2)) with potent analgesic activity."( Synthesis of dermorphin-(1-4) derivatives catalyzed by proteases in organic solvents.
Shen, HY; Tian, GL; Ye, YH, 2005
)
1.42
"Dermorphin is an exceptionally potent opioid peptide from amphibian skin. "( Dermorphin: effects on anterior pituitary function in the rat.
Güllner, HG; Kelly, GD, 1983
)
3.15
"Dermorphin is a recently discovered opioid peptide which is unique in having a D-amino acid in its sequence. "( Effect of dermorphin and morphine on the sympathetic and cardiovascular system of the pithed rat.
Feuerstein, G; Zukowska-Grojec, Z,
)
1.98
"Dermorphin (D) is a potent opiate-like peptide isolated from the skin of some species of frogs. "( Dermorphin inhibits spinal nociceptive flexion reflex in humans.
Degli Uberti, EC; Margutti, A; Nappi, G; Pansini, R; Salvadori, S; Sandrini, G; Tomatis, R; Trasforini, G, 1986
)
3.16
"Dermorphin is an opioid peptide containing one D-amino acid isolated from amphibian skin. "( Dermorphin-like immunoreactivity in guinea pig and rat stomach.
Tang, YQ; Tsou, K; Wang, FS; Wang, SH, 1985
)
3.15

Effects

Dermorphin binding sites have been shown in central and peripheral organs. Central administered dermorphin produces profound autonomic responses. Dermorphin has little in common with the sequence of all hitherto known mammalian opioid peptides.

ExcerptReferenceRelevance
"Dermorphin, in its turn, has been found to cause, by intracerebroventricular injection, not only analgesia and catalepsy, but also conspicuous EEG and behavioral changes in the rabbit and chick, as well as a sharp reduction in gastric emptying time and gastric acid output in the rat, together with marked stimulation of PRL release."( The brain-gut-skin triangle: new peptides.
Broccardo, M; Erspamer, GF; Erspamer, V; Falaschi, P; Improota, G; Melchiorri, P; Negri, L; Renda, T, 1981
)
0.98
"Dermorphin has little in common with the sequence of all hitherto known mammalian opioid peptides and is unique in having a D-amino acid residue in position 2."( Characterization of the receptor binding profile of (3H)-dermorphin in the rat brain.
Amiche, M; Delfour, A; Mor, A; Nicolas, P; Sagan, S, 1988
)
1.24
"Dermorphin binding sites have been shown in central and peripheral organs and central administered dermorphin produces profound autonomic responses."( Effect of dermorphin and morphine on the sympathetic and cardiovascular system of the pithed rat.
Feuerstein, G; Zukowska-Grojec, Z,
)
1.26

Actions

ExcerptReferenceRelevance
"dermorphin but the increase in urinary sodium excretion produced by this antagonist was converted to an antinatriuresis."( Central mu opioids mediate differential control of urine flow rate and urinary sodium excretion in conscious rats.
Dzialowski, EM; Kapusta, DR, 1995
)
1.01

Toxicity

ExcerptReferenceRelevance
" Taken together, these data would suggest that this selective ablation of mu opioid receptor bearing descending facilitatory neurons in the RVM with dermorphin-saporin did not elicit the long-standing evident adverse toxicity in terms of some physiological parameters and neurochemical alterations we determined, plausibly providing us a safe and reliable approach to treat some intractable pain."( Evaluation of side effects through selective ablation of the mu opioid receptor expressing descending nociceptive facilitatory neurons in the rostral ventromedial medulla with dermorphin-saporin.
Cao, F; Chen, SS; Chen, ZJ; Gao, F; Liu, XJ; Tian, YK; Xiao, XP; Xu, AJ; Yan, XF; Yang, H; Yang, SB, 2009
)
0.75

Bioavailability

ExcerptReferenceRelevance
" Bioavailability following intramuscular administration was variable (47-100%, n = 3)."( Pharmacokinetics and pharmacodynamics of dermorphin in the horse.
Guan, F; McDonnell, S; Robinson, MA; Soma, LR; Uboh, CE, 2015
)
0.68

Dosage Studied

The dose-response curves of [Lys7]dermorphin antinociception were shifted to the right by the pretreatment with naloxone. Microinjection of dynamin-DN and ConA also decreased the ant inociceptive potency of the unlabeled opioid agonist dermorphin.

ExcerptRelevanceReference
" In these experiments, dose-response curves were recorded."( New models for the evaluation of opioid effects in the guinea-pig ileum.
Donnerer, J; Lembeck, F, 1985
)
0.27
" at a dosage 1000 times lower than that of morphine on a molar basis."( Comparative study on the electrophysiological responses at thalamic level to different analgesic peptides.
Biella, G; Braga, PC; Fraschini, F; Guidobono, F; Pecile, A; Tiengo, M, 1985
)
0.27
" The dose-response curves of [Lys7]dermorphin antinociception were shifted to the right by the pretreatment with naloxone (0."( Production of antinociception by peripheral administration of [Lys7]dermorphin, a naturally occurring peptide with high affinity for mu-opioid receptors.
Lattanzi, R; Melchiorri, P; Negri, L, 1995
)
0.8
" The decreases in labeling index evoked by OGF were blocked by concomitant administration of the opioid antagonist, naloxone (10 mg/kg); naloxone alone at the dosage utilized had no influence on cell replicative processes."( The opioid growth factor, [Met5]-enkephalin, and the zeta opioid receptor are present in human and mouse skin and tonically act to inhibit DNA synthesis in the epidermis.
McLaughlin, PJ; Wu, Y; Zagon, IS, 1996
)
0.29
" At the dosage used, naltrindole occupied more than 98% of brain delta-opioid receptors without affecting mu-opioid-receptors."( Interaction between the mu-agonist dermorphin and the delta-agonist [D-Ala2, Glu4]deltorphin in supraspinal antinociception and delta-opioid receptor binding.
Improta, G; Lattanzi, R; Luchetti, F; Melchiorri, P; Negri, L; Potenza, RL, 1995
)
0.57
" TAPA dose-response curve for antinociception."( Selective antagonism by naloxonazine of antinociception by Tyr-D-Arg-Phe-beta-Ala, a novel dermorphin analogue with high affinity at mu-opioid receptors.
Hayashi, T; Kisara, K; Kutsuwa, M; Sakurada, C; Sakurada, S; Sakurada, T; Sato, T; Takeda, S; Tan-No, K; Yuki, M, 2000
)
0.53
" Microinjection of dynamin-DN and ConA also decreased the antinociceptive potency of the unlabeled opioid agonist dermorphin when microinjected into the vlPAG as demonstrated by rightward shifts in the dose-response curves."( Opioid receptor internalization contributes to dermorphin-mediated antinociception.
Aicher, SA; Arttamangkul, S; Bobeck, EN; Hegarty, DM; Ingram, SL; Macey, TA; Morgan, MM, 2010
)
0.83
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-P receptorRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00010.19930.3981AID145798
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.03890.00010.729810.0000AID148639; AID1504682; AID1872068
Delta-type opioid receptorMus musculus (house mouse)Ki1.00400.00000.53939.4000AID149091
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.13400.00000.60689.2330AID149804
Kappa-type opioid receptorMus musculus (house mouse)IC50 (µMol)1.00000.00131.538010.0000AID1872069
Mu-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00430.00010.887410.0000AID1504686; AID151456
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00070.00000.38458.6000AID151758
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00180.00010.813310.0000AID1504686; AID152086; AID440034; AID621164
Mu-type opioid receptorHomo sapiens (human)Ki0.00720.00000.419710.0000AID1268024; AID1268040; AID1872031
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)0.24920.00020.75218.0140AID149633; AID1504687; AID440035; AID621165
Delta-type opioid receptorHomo sapiens (human)Ki0.92900.00000.59789.9300AID1872032
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)10.00000.00030.71237.0700AID148678
Kappa-type opioid receptorHomo sapiens (human)Ki8.16200.00000.362410.0000AID1872033
Nociceptin receptorHomo sapiens (human)IC50 (µMol)10.00000.00010.12532.2000AID271065
Mu-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.00860.00081.699210.0000AID1872058; AID1872067
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00260.00020.660310.0000AID1504681; AID1872057; AID224723
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.07350.00000.32639.4000AID1676256; AID1676258; AID375522
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

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)
calcium-mediated signalingNociceptin receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
sensory perceptionNociceptin receptorHomo sapiens (human)
sensory perception of painNociceptin receptorHomo sapiens (human)
response to estradiolNociceptin receptorHomo sapiens (human)
positive regulation of urine volumeNociceptin receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayNociceptin receptorHomo sapiens (human)
eating behaviorNociceptin receptorHomo sapiens (human)
negative regulation of cAMP-mediated signalingNociceptin receptorHomo sapiens (human)
estrous cycleNociceptin receptorHomo sapiens (human)
negative regulation of blood pressureNociceptin receptorHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
regulation of locomotor rhythmNociceptin receptorHomo sapiens (human)
conditioned place preferenceNociceptin receptorHomo sapiens (human)
neuropeptide signaling pathwayNociceptin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

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)
nociceptin receptor activityNociceptin receptorHomo sapiens (human)
G protein-coupled receptor activityNociceptin receptorHomo sapiens (human)
protein bindingNociceptin receptorHomo sapiens (human)
neuropeptide bindingNociceptin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

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 membraneNociceptin receptorHomo sapiens (human)
cytoplasmic vesicleNociceptin receptorHomo sapiens (human)
plasma membraneNociceptin receptorHomo sapiens (human)
neuron projectionNociceptin receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (112)

Assay IDTitleYearJournalArticle
AID25949Half-life of the compound1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID1872065Antinociceptive activity in rat2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1676259Potency index, ratio of EC50 for N/OFQ(1-13)-NH2 to EC50 for test compound for agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incuba
AID151609Binding affinity against Opioid receptor mu 1 using [3H]DAMGO in rat brain synaptosomes was determined2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
AID138349In vitro concentration required to inhibit electrically evoked twitch in isolated mouse vas deferens.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
AID1872064Antinociceptive activity in mouse by tail pressure test2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID375529Antagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilization at up to 10 uM2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
AID149340Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and structure-activity relationships of deltorphin analogues.
AID710806Antinociceptive activity in CD1 mouse assessed as AUC of thermal-stimulus induced tail flick latency assessed per min at 1 umol/kg, ip up to 120 mins2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
AID1872032Binding affinity to DOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID149743In vitro biological activity by electrically induced smooth muscle contractions in guinea pig ileum (Opioid receptor mu 1); inhibitory concentration was evaluated2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
AID108533Antinociceptive activity after subcutaneous administration in mice.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
AID148639In vitro biological activity by electrically induced smooth muscle contractions in mouse vas deferens (Opioid receptor delta 1); inhibitory concentration was evaluated2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
AID256773Functional bioactivity against delta opioid receptor in mouse vas deferens2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID148991Inhibition of opioid receptor mu in guinea pig ileum (GPI)1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and structure-activity relationships of deltorphin analogues.
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.
AID440034Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells after 90 mins by scintillation counting2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
AID132805In vivo analgesic activity in the mouse tail-flick assay following s.c. administration.1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID149339Displacement of [3H]- DPDPE from delta opioid receptor in rat brain membrane1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and structure-activity relationships of deltorphin analogues.
AID148678Evaluated for the inhibition of [3H]EKC binding to Opioid receptor kappa 1 of guinea pig brain1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID149935Opioid receptor delta 1 binding affinity by displacement of radioligand [3H][D-Pen]-enkephalin (DPDPE) from rat brain membrane synaptosomes1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
AID440035Displacement of [3H]DPDPE from delta opioid receptor expressed in CHO cells after 90 mins by scintillation counting2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
AID145798Affinity for rat Tachykinin receptor 1 determined in displacement screening by using radioligand 3,4-[3H]-(L-Pro e2) SP.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.
AID73682In vitro inhibitory activity against electrically evoked contractions of guinea pig ileum (GPI)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID149633Evaluated for the inhibition of [3H]DADLE binding to Opioid receptor delta 1 of guinea pig brain1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID1268024Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexy2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.
AID440037Selectivity ratio of IC50 for delta opioid receptor to IC50 for mu opioid receptor2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
AID239304Inhibition of [3H]naloxone binding to rat brain homogenate Opioid receptor delta2005Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
AID138840Agonist activity at mu receptor as maximal effect induced by an agonist expressed as percent inhibition of the electrically induced twitches in guinea pig ileum2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.
AID621165Agonist activity at delta-type opioid receptor2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis, biological evaluation, and automated docking of constrained analogues of the opioid peptide H-Dmt-D-Ala-Phe-Gly-NH₂ using the 4- or 5-methyl substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one scaffold.
AID23167Half-life time of enzymatic breakdown in mouse liver.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
AID149310IC50 ratio is GPI/MVD1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and structure-activity relationships of deltorphin analogues.
AID1504687Binding affinity to delta-type opioid receptor (unknown origin)
AID229344Ratio of inhibitory concentration of mouse vas deferens to guinea pig ileum was determined2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
AID148609In vitro inhibitory activity against opioid activity in guinea pig ileum, relative to Morphine1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
AID232685Selectivity ratio of IC50 of mu receptor to IC50 of delta receptor1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID137100Relative potency was determined for the compound with respect to morphine activity (1) after icv administration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID136966In vivo analgesic potency in mice compared to morphine after s.c. administration.1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID131166Compound was tested in vivo by a mouse tail-flick assay after subcutaneous (sc) injection1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
AID132288The compound was evaluated for the analgesic activity by tail-flick test after icv administration of compound in mouse; value ranges from 6.6-27.11987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID621164Agonist activity at Mu-type opioid receptor2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis, biological evaluation, and automated docking of constrained analogues of the opioid peptide H-Dmt-D-Ala-Phe-Gly-NH₂ using the 4- or 5-methyl substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one scaffold.
AID151268Displacement of [3H]-DAGO from Opioid receptor mu 1 of adult male mouse brain.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
AID79023In vitro concentration required to inhibit electrically evoked twitch in isolated guinea pig ileum.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
AID26438Half-life was determined1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID151456The compound was tested for binding affinity towards [3H]DAMGO, in rat Opioid receptor mu 11999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.
AID148608In vitro inhibitory activity against opioid activity in guinea pig ileum1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
AID256771Displacement of [3H]DAMGO from rat mu opioid receptor in brain P2 synaptosomes2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID239267Inhibition of [3H]naloxone binding to rat brain homogenate Opioid receptor mu2005Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
AID151746Inhibition of [3H]DAGO binding to Opioid receptor mu 1 of rat brain P2 synaptosomes2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID1504682Agonist activity at delta-type opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated contractions
AID1872071Antinociceptive activity in mouse administered iv by hot plate test2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1872058Antagonist activity at mouse vas deferns MOP2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID147933Relative potency with respect to morphine was evaluated for Opioid receptor delta 1 of guinea pig brain1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID1268040Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.
AID132582In Vivo opioid activity was evaluated by determining analgesia in the mouse by the tail-flick test when administered through intra cerebro ventricular route1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
AID1872106Toxicity in rat assessed as antinociceptive activity tolerance at 3 to10 nmol/kg measured after 5 days with 62 pmol/h icv infusion relative to control2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID224723Evaluated for the inhibition of [3H]DAGO binding to mu-receptor of guinea pig brain1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID73189Negative logarithm of the molar concentration of an agonist to produce 50% of the maximum effect in guinea pig ileum (mu receptor) determined2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID256770Displacement of [3H]deltorphin II from rat delta opioid receptor in brain P2 synaptosomes2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID271064Displacement of [3H]DAMGO from mu opioid receptor in rat brain homogenate2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide.
AID149204In vitro opioid receptor delta mediated mouse vas deferens (MVD) assay1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and structure-activity relationships of deltorphin analogues.
AID1676256Agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
AID224724Relative potency with respect to morphine was evaluated for mu-receptor of guinea pig brain1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID1504686Binding affinity to Mu-type opioid receptor (unknown origin)
AID228359Ratio of delta-Opioid receptor to the mu-opioid receptor1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
AID1872070Antinociceptive activity in rat administered icv2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID78861Bioactivity in vitro in guinea pig ileum (GPI) isolated organ preparation1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
AID130360In vivo analgesic activity in the mouse tail-flick assay following i.c.v. administration.1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID150100The selectivity ratio as the ratio of Ki of Opioid receptor delta 1 to Ki of Opioid receptor mu 12002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
AID1872031Binding affinity to MOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID149091Displacement of [3H]NLT from Opioid receptor delta 1 of adult male mouse brain.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
AID112941Analgesic activity in mice by using hot plate method1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Structure-activity studies of dermorphin. Synthesis and some pharmacological data of dermorphin and its 1-substituted analogues.
AID77502Relative potency compared to Morphine in electrically stimulated guinea pig ileum.1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID136970In vivo opioid activity was evaluated by determining analgesia in the mouse by the tail-flick test, relative potency with respect to morphine intra cerebro ventricular route1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
AID1872068Antagonist activity at mouse brain homogenate DOP2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1872069Antagonist activity at mouse brain homogenate KOP2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1504681Agonist activity at mu-opioid receptor in guinea pig ileum assessed as inhibition of electrically induced contractions
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.
AID137101Relative potency was determined for the compound with respect to morphine activity (1) after subcutaneous administration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID149290Displacement of [3H]- DAGO from opioid receptor mu in rat brain membrane1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and structure-activity relationships of deltorphin analogues.
AID149792Inhibition of [3H]DPDPE binding to Opioid receptor delta 1 of rat brain P2 synaptosomes2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID152086Agonist activity for Opioid receptor mu 11997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.
AID136973In vivo opioid activity was evaluated by determining analgesia in the mouse by the tail-flick test. Relative potency with respect to morphine when administered through subcutaneous route1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
AID148203Negative logarithm of the molar concentration for agonist activity at mu receptor was determined in guinea pig ileum2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.
AID1676260Bias factor, selectivity for agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation to agonist activity at NOP (unknown origin) expressed in
AID77501Inhibition of electrically evoked twitches in guinea pig ileum relative to morphine.1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Structure-activity studies of dermorphin. Synthesis and some pharmacological data of dermorphin and its 1-substituted analogues.
AID1676257Potency index, ratio of EC50 for N/OFQ(1-13)-NH2 to EC50 for test compound for agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mi
AID1872057Antagonist activity at guinea pig ileum MOP2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
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.
AID148482In vitro opioid inhibitory activity against in guinea pig ileum1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
AID149670Binding affinity against Opioid receptor delta 1 using [3H]DT in rat brain synaptosomes was determined2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
AID1676258Agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
AID151611Binding affinity for rat brain P2 synaptosome Opioid receptor mu 12002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID149672Binding affinity at Opioid receptor delta 1 using rat brain receptor (P2 synaptosome) assay2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID1872067Antagonist activity at mouse brain homogenate MOP2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID125450In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID23166Half-life time of enzymatic breakdown in mouse brain.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
AID271065Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide.
AID149311Relative affinity for mu and delta opioid receptors in rat brain membrane1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and structure-activity relationships of deltorphin analogues.
AID234756Relative binding to mu and delta opioid receptors (ratio of Ki)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID1872033Binding affinity to KOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID136965In vivo analgesic potency in mice compared to morphine after i.c.v. administration.1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID151895Opioid receptor mu 1 binding affinity by displacement of radioligand [3H][DAla,MePhe,Gly-ol]enkephalin (DAGO) from rat brain membrane synaptosomes1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
AID132297The compound was evaluated for the analgesic activity by tail-flick test after subcutaneous administration of compound in mouse; value ranges from 1.73-6.41987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
AID76090Inhibition of twitches in guinea pig ileum1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Structure-activity studies of dermorphin. Synthesis and some pharmacological data of dermorphin and its 1-substituted analogues.
AID1872077Antinociceptive activity in mouse administered icv2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID256772Selectivity for rat mu opioid receptor over delta opioid receptor2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID256774Functional bioactivity against mu opioid receptor in guinea-pig ileum2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID131044Compound was tested in vivo by a mouse tail-flick assay after intracerebroventricular (icv) injection1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
AID375522Antagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilization2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
AID78310In vitro inhibition of contractions in the electrically stimulated guinea pig ileum.1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
AID1872072Antinociceptive activity in mouse administered IV2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (365)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990147 (40.27)18.7374
1990's118 (32.33)18.2507
2000's58 (15.89)29.6817
2010's34 (9.32)24.3611
2020's8 (2.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.69

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.69 (24.57)
Research Supply Index6.00 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index62.62 (26.88)
Search Engine Supply Index2.05 (0.95)

This Compound (39.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (0.50%)5.53%
Reviews11 (2.74%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other388 (96.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]