Page last updated: 2024-11-12

dynorphins

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Description

Dynorphins: A class of opioid peptides including dynorphin A, dynorphin B, and smaller fragments of these peptides. Dynorphins prefer kappa-opioid receptors (RECEPTORS, OPIOID, KAPPA) and have been shown to play a role as central nervous system transmitters. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

dynorphin (1-13): potent opioid peptide; see also record for dynorphin & D-Ala(2)-dynorphin (1-11) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16129685
MeSH IDM0006908
PubMed CID25075996
CHEMBL ID405618
MeSH IDM0006908

Synonyms (41)

Synonym
dynorphin
74913-18-1
dynorphins
yggflrrxrpklkwdnq
bdbm224025
gtpl1619
dinorphin a (1-13)
1-13-dynorphin a (swine)
dynorphin a (1-13)
dynorphin (1-13)
l-lysine, l-tyrosylglycylglycyl-l-phenylalanyl-l-leucyl-l-arginyl-l-arginyl-l-isoleucyl-l-arginyl-l-prolyl-l-lysyl-l-leucyl-
dynorphin 1-13
NCGC00163681-01
NCGC00163681-02
tyr-gly-gly-phe-leu-arg-arg-ile-arg-pro-lys-leu-lys(dynorphin a(1-13)amide)
bdbm50241435
dynorphin(1-13)-oh
dynorphin a 1-13
CHEMBL405618 ,
dynorphin-(1-13)
dynorphin a1-13
dynorphin a(1-13)
72957-38-1
unii-vfc23v742z
vfc23v742z ,
porcine dynorphin a(1-13)
dynorphin a (1-13), porcine
mfcd00076366
bdbm214798
yggflrrirpklk
dynorphin a (1-13) h-tyr-gly-gly-phe-leu-arg-arg-ile-arg-pro-lys-leu-lys-oh
dynorphin 1-13 [mi]
dynorphin a 1-13 human
dyn a(1-13)-oh
1-13-dynorphin a (pig)
yggflrrxrpklk
bdbm224024
porcine dynorphin a 1-13
porcinedynorphina(1-13)
AS-76942
AKOS040763911

Research Excerpts

Overview

Dynorphins (dyn) are a major class of endogenous opioid peptides. They modulate the functions of immune cells.

ExcerptReferenceRelevance
"Dynorphins (dyn) are a major class of endogenous opioid peptides that modulate the functions of immune cells. "( Inhibition of lipopolysaccharide-induced nitric oxide and cytokine production by ultralow concentrations of dynorphins in mixed glia cultures.
Hong, JS; Hudson, PM; Jin, L; Kong, LY; McMillian, MK, 1997
)
1.95

Actions

ExcerptReferenceRelevance
"Dynorphins produce neural excitation and excitotoxic effects in the spinal cord through a kappa-opioid facilitation of NMDA receptor-sensitivity to glutamate."( Bi-phasic intensity-dependent opioid-mediated neural amplitude changes in the chinchilla cochlea: partial blockade by an N-Methyl-D-Aspartate (NMDA)-receptor antagonist.
Anderson, DJ; Chernicky, CL; Sahley, TL, 2008
)
1.07

Toxicity

ExcerptReferenceRelevance
" Thus, the toxic effects were structure selective but not mediated through opioid receptors."( Cytotoxic effects of dynorphins through nonopioid intracellular mechanisms.
Aguilar-Santelises, M; Bakalkin, G; Cebers, G; Gileva, I; Hauser, KF; Hoon Goh, B; Reznikov, K; Tan-No, K; Terenius, L; Yakovleva, T, 2001
)
0.63
" R6W and wt Dyn A peptides were most toxic to primary cerebellar neurons."( Altered secondary structure of Dynorphin A associates with loss of opioid signalling and NMDA-mediated excitotoxicity in SCA23.
Bakalkin, G; Dooley, C; Marrink, SJ; McLaughlin, J; Melo, MN; Reits, E; Sinke, RJ; Smeets, CJ; Stargardt, A; Verbeek, DS; Zmorzyńska, J, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" However, in both cases, levels of corticosterone in plasma were dramatically elevated, clearly demonstrating the bioavailability of the kappa agonists."( The endogenous kappa agonist, dynorphin(1-13), does not alter basal or morphine-stimulated dopamine metabolism in the nigrostriatal pathway of the rat.
Cosi, C; Iyengar, S; Kim, HS; Wood, PL, 1987
)
0.27
" However, in both cases, levels of corticosterone in plasma were dramatically elevated, clearly demonstrating the bioavailability of the kappa agonists."( The endogenous kappa agonist, dynorphin(1-13), does not alter basal or morphine-stimulated dopamine metabolism in the nigrostriatal pathway of the rat.
Cosi, C; Iyengar, S; Kim, HS; Wood, PL, 1987
)
0.27

Dosage Studied

ExcerptRelevanceReference
" In the small dosage groups (0."( [Effects of the dynorphin derivative "E2078" on hemodynamics and plasma catecholamines in dogs].
Hirota, K, 1990
)
0.28
" However, the dose-response curve for the substance P effect had a biphasic shape."( Differential modulation of striatal dopamine release by intranigral injection of gamma-aminobutyric acid (GABA), dynorphin A and substance P.
Herrera-Marschitz, M; Hökfelt, T; Reid, M; Terenius, L; Ungerstedt, U, 1988
)
0.27
" For blood pressure and heart rate, pretreatment with a midportion beta-endorphin antiserum resulted in a parallel shift to the right of the dose-response curve for alpha-methyldopa."( Possible involvement of beta endorphin(1-31) and dynorphin(1-13) in the central hypotensive mechanism of action of alpha methyldopa.
de Jong, W; van Giersbergen, PL; Wiegant, VM, 1989
)
0.28
", DPDPE displaced the morphine dose-response line to the left and also potentiated the effects of normorphine and etorphine."( Differential modulation by [D-Pen2, D-Pen5]enkephalin and dynorphin A-(1-17) of the inhibitory bladder motility effects of selected mu agonists in vivo.
Nunan, L; Porreca, F; Sheldon, RJ, 1989
)
0.28
" Slightly conflicting results have been obtained, depending on the dosage of naloxone used."( Endorphins: what are they? How are they measured? What is their role in exercise?
Grossman, A; Sutton, JR, 1985
)
0.27
" There is an inverse dose-response relation for PMN but not PMO."( Opioid peptides rapidly stimulate superoxide production by human polymorphonuclear leukocytes and macrophages.
Gekker, G; Keane, WF; Peterson, PK; Sharp, BM; Suh, HJ; Tsukayama, D, 1985
)
0.27
" Dose-response curves for the relatively specific ligands for the mu-, kappa-, and sigma-receptors were determined using morphine (mu-receptors), dynorphin-(1-13) (kappa-receptors), and N-allylnormetazocine (sigma-receptors)."( Sites of action of mu-, kappa- and sigma-opiate receptor agonists at the feline ileocecal sphincter.
Cohen, S; Ouyang, A; Vos, P, 1988
)
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
" A particular application of this method was exemplified by the dosage of enkephalins secreted from perfused bovine adrenal glands."( Sensitive method of detection, quantitation and purification of peptides using pre-column derivatization with phenyl isothiocyanate.
Dumont, M; Lemaire, S; Nolet, S, 1988
)
0.27
" Similar blockade was observed for EKC and U 50488 at doses of 10 and/or 20 ng/kg, but DAGO was unable to affect the AS-induced gastric inhibition at any dosage tested (20-200 ng/kg icv)."( CNS blockade of acoustic stress-induced gastric motor inhibition by kappa-opiate agonists in dogs.
Alvinerie, M; Bueno, L; Gue, M; Honde, C; Junien, JL; Pascaud, X, 1988
)
0.27
" Although the group X dosage interaction was not significant, an internally consistent tendency effect of naloxone among the different treatment groups was observed."( The effect of ovariectomy, estradiol and progesterone on opioid modulation of feeding.
Gosnell, BA; Grace, M; Kneip, J; Levine, AS; Morley, JE, 1984
)
0.27
" Naloxone also caused a rightward shift of the dose-response curve for dynorphin A, suggesting a competitive antagonism mechanism."( Identification of dynorphins as endogenous ligands for an opioid receptor-like orphan receptor.
Yu, L; Zhang, S, 1995
)
0.63
"Quantitative in situ hybridization histochemistry was used to compare the effects of AMPH administration on mRNAs coding for zif/268, a member of the zinc finger family of immediate early genes, and the opioid peptides, preprodynorphin (PPD) and preproenkephalin (PPE), in rat striatum after 3 dosing schedules: (1) acute; (2) once a day for 5 days, and (3) once a day for 5 days followed 10 days later by a challenge dose."( Alterations in striatal zif/268, preprodynorphin and preproenkephalin mRNA expression induced by repeated amphetamine administration in rats.
McGinty, JF; Wang, JQ, 1995
)
0.29
" However, the response of preproenkephalin, c-fos and zif/268 mRNAs to such a dosing regimen is unknown."( Cocaine binges differentially alter striatal preprodynorphin and zif/268 mRNAs.
Daunais, JB; McGinty, JF, 1995
)
0.29
" We have further investigated the non-opioid nature of this activity by comparing the efficacies of dyn A(1-13) and (2-17) under different experimental protocols with a variety of dosing regimens."( Dynorphin A modulates acute and chronic opioid effects.
He, L; Hooke, LP; Lee, NM, 1995
)
0.29
" Naloxone shifted to the right the dose-response curves for each opioid peptide significantly enhancing the ED50 values."( Modulation of non-adrenergic non-cholinergic inhibitory transmission in rat duodenum: role of opiates and 5-hydroxytryptamine.
Adamo, EB; Di Giovanni, G; Marini, R; Mulè, F; Postorino, A; Serio, R, 1993
)
0.29
" In the present study, dose-response effects of acute administration of these stimulants on preproenkephalin (PPE) mRNA expression in the rat striatum were investigated with quantitative in situ hybridization histochemistry 3 h after injection."( D1 and D2 receptor regulation of preproenkephalin and preprodynorphin mRNA in rat striatum following acute injection of amphetamine or methamphetamine.
McGinty, JF; Wang, JQ, 1996
)
0.29
" There were four volunteers receiving long-term opioid therapy and six opioid-naive volunteers (nonopioid group) within each dosing group."( Pharmacokinetics of intravenous dynorphin A(1-13) in opioid-naive and opioid-treated human volunteers.
Billard, V; Brose, WG; Gambús, PL; Hochhaus, G; Minto, CF; Schnider, TW; Shafer, SL; Youngs, EJ, 1998
)
0.3
" Morphine analgesia was inhibited by dynorphin as shown by a rightward shift of the morphine dose-response curve."( Antianalgesic action of dynorphin A mediated by spinal cholecystokinin.
Fujimoto, JM; Holmes, BB; Rady, JJ, 1999
)
0.3
" Dose-response curves constructed from the data indicated that the antinociceptive effect of nitrous oxide was significantly antagonized by antisera to various dynorphins (DYNs) and methionine-enkephalin (ME), but not by antiserum to beta-endorphin (beta-EP)."( Antagonism of nitrous oxide antinociception in mice by intrathecally administered antisera to endogenous opioid peptides.
Cahill, FJ; Ellenberger, EA; Mueller, JL; Quock, RM; Tseng, LF,
)
0.33
" Because its pharmacological characterization has not been fully identified, the present study examined whether a dose-response range of general and selective opioid antagonists as well as antisense oligodeoxynucleotide (AS ODN) opioid probes altered daytime feeding over a 4-h time course elicited by dynorphin."( Dynorphin A(1-17)-induced feeding: pharmacological characterization using selective opioid antagonists and antisense probes in rats.
Bodnar, RJ; Grossman, HC; Hadjimarkou, MM; Pasternak, GW; Rossi, GC; Silva, RM, 2002
)
0.31
" Antinociceptive dose-response curves were constructed for spinal Delta(9)-THC and WIN 55,212-2 in prodynorphin knock-out mice and in wild-type littermates."( Dynorphin-independent spinal cannabinoid antinociception.
Gardell, LR; Lai, J; Ossipov, MH; Porreca, F; Vanderah, TW, 2002
)
0.31
" Studies began one hour before methadone dosing to avoid the expected increase in prolactin that coincides with peak plasma levels of methadone."( Suppressed prolactin response to dynorphin A1-13 in methadone-maintained versus control subjects.
Bart, G; Borg, L; Green, M; Ho, A; Kreek, MJ; Schluger, JH, 2003
)
0.32
" A dose-response study with the selective kappa antagonist nor-binaltorphimine (nor-BNI) showed that a low dose (1."( The dynamic relationship between mu and kappa opioid receptors in body temperature regulation.
Adler, MW; Chen, X; Geller, EB; McClatchy, DB; Tallarida, RJ, 2005
)
0.33
" Ablation of NK-1 receptor expressing cells prevented (a) morphine-induced thermal and mechanical hypersensitivity, (b) increased touch-evoked spinal FOS expression, (c) upregulation of spinal dynorphin content and (d) the rightward displacement of the spinal morphine antinociceptive dose-response curve (i."( Spinal NK-1 receptor expressing neurons mediate opioid-induced hyperalgesia and antinociceptive tolerance via activation of descending pathways.
King, T; Lai, J; Ossipov, MH; Porreca, F; Vanderah, TW; Vera-Portocarrero, LP; Zhang, ET, 2007
)
0.34
" When PHN pain intensity returned to baseline and/or at patients' first request for rescue analgesia other than acetaminophen (typically around 28 days after dosing but sometimes as soon as two days postdose), patients were to cross over to the alternative treatment and be monitored on the same schedule."( A Phase II, multicenter, randomized, double-blind, placebo-controlled crossover study of CJC-1008--a long-acting, parenteral opioid analgesic--in the treatment of postherpetic neuralgia.
Castaigne, JP; Clark, AJ; Morley-Forster, P; Moulin, D; Neale, A; Teichman, S; Wallace, MS; Wasserman, R,
)
0.13
" Dose-response and time course curves were done."( Role of nociceptin/orphanin FQ and the pseudopeptide [Phe1Psi(CH2NH)Gly2]-nociceptin(1-13)-NH2 and their interaction with classic opioids in the modulation of thermonociception in the land snail Helix aspersa.
Cruz, SL; León-Olea, M; Miller-Pérez, C; Pellicer, F; Rodríguez-Manzo, G; Sánchez-Islas, E, 2008
)
0.35
" Here, we used clinically relevant dosing to examine the effects of maternally administered sustained-release naltrexone on the rat brain by examining offspring at birth and in adulthood."( Maternally administered sustained-release naltrexone in rats affects offspring neurochemistry and behaviour in adulthood.
Dunlop, SA; Farid, WO; Hulse, GK; Krstew, EV; Lawrence, AJ; Tait, RJ, 2012
)
0.38
" The effects of the PIs on antinociception and toxicity were evaluated by a dose-response study and a comparison of differences among various combinations of Dyn A (1-17) or Dyn A (1-13) and the three PIs and p-hydroxymercuribenzoate."( Effect of three peptidase inhibitors on antinociceptive potential and toxicity with intracerebroventricular administration of dynorphin A (1-17) or (1-13) in the rat.
Ajimi, J; Kawaguchi, M; Kobayashi, H; Miura, M; Suzuki, T; Takahashi, S; Tsukamoto, H; Yoshikawa, M, 2015
)
0.42
" For blood pressure and heart rate, pretreatment with a midportion beta-endorphin antiserum resulted in a parallel shift to the right of the dose-response curve for alpha-methyldopa."( Possible involvement of beta endorphin(1-31) and dynorphin(1-13) in the central hypotensive mechanism of action of alpha methyldopa.
de Jong, W; van Giersbergen, PL; Wiegant, VM, 1989
)
0.28
" A particular application of this method was exemplified by the dosage of enkephalins secreted from perfused bovine adrenal glands."( Sensitive method of detection, quantitation and purification of peptides using pre-column derivatization with phenyl isothiocyanate.
Dumont, M; Lemaire, S; Nolet, S, 1988
)
0.27
" We have further investigated the non-opioid nature of this activity by comparing the efficacies of dyn A(1-13) and (2-17) under different experimental protocols with a variety of dosing regimens."( Dynorphin A modulates acute and chronic opioid effects.
He, L; Hooke, LP; Lee, NM, 1995
)
0.29
" There were four volunteers receiving long-term opioid therapy and six opioid-naive volunteers (nonopioid group) within each dosing group."( Pharmacokinetics of intravenous dynorphin A(1-13) in opioid-naive and opioid-treated human volunteers.
Billard, V; Brose, WG; Gambús, PL; Hochhaus, G; Minto, CF; Schnider, TW; Shafer, SL; Youngs, EJ, 1998
)
0.3
" Dose-response curves constructed from the data indicated that the antinociceptive effect of nitrous oxide was significantly antagonized by antisera to various dynorphins (DYNs) and methionine-enkephalin (ME), but not by antiserum to beta-endorphin (beta-EP)."( Antagonism of nitrous oxide antinociception in mice by intrathecally administered antisera to endogenous opioid peptides.
Cahill, FJ; Ellenberger, EA; Mueller, JL; Quock, RM; Tseng, LF,
)
0.13
" When PHN pain intensity returned to baseline and/or at patients' first request for rescue analgesia other than acetaminophen (typically around 28 days after dosing but sometimes as soon as two days postdose), patients were to cross over to the alternative treatment and be monitored on the same schedule."( A Phase II, multicenter, randomized, double-blind, placebo-controlled crossover study of CJC-1008--a long-acting, parenteral opioid analgesic--in the treatment of postherpetic neuralgia.
Castaigne, JP; Clark, AJ; Morley-Forster, P; Moulin, D; Neale, A; Teichman, S; Wallace, MS; Wasserman, R,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency22.38720.003245.467312,589.2998AID2517
phosphopantetheinyl transferaseBacillus subtilisPotency89.12510.141337.9142100.0000AID1490
regulator of G-protein signaling 4Homo sapiens (human)Potency0.00530.531815.435837.6858AID504845
DNA polymerase kappa isoform 1Homo sapiens (human)Potency33.58750.031622.3146100.0000AID588579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00340.00010.601710.0000AID55440
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.00770.00010.729810.0000AID226081; AID749871
Kappa-type opioid receptorMus musculus (house mouse)Ki0.00030.00030.35942.7500AID1773070
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00400.00000.38458.6000AID749873
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki0.00150.00000.18683.9500AID148576; AID55440; AID65519; AID65522
Mu-type opioid receptorHomo sapiens (human)Ki0.00800.00000.419710.0000AID1714329
Delta-type opioid receptorHomo sapiens (human)Ki0.01150.00000.59789.9300AID147916; AID149887; AID150045; AID1714330; AID749872
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00110.00000.20186.4240AID148103; AID149137
Kappa-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00010.00001.201110.0000AID1714328
Kappa-type opioid receptorHomo sapiens (human)Ki0.28350.00000.362410.0000AID1714328; AID1802456; AID219259
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.01470.00000.27869.0000AID147916; AID149021; AID749873
[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)
Mas-related G-protein coupled receptor member X2Homo sapiens (human)EC50 (µMol)11.65000.14003.73818.9000AID1802708; AID1802709
Kappa-type opioid receptorMus musculus (house mouse)EC50 (µMol)0.08280.00080.80564.8860AID1773069; AID1773078
Kappa-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.01070.00040.00390.0180AID148443; AID55438; AID65520
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.21380.00000.32639.4000AID1275489; AID1279232
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)0.01860.00000.43328.3000AID1275490; AID1279233
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.01800.00000.20671.4454AID148736
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.11690.00000.22448.9900AID1256748; AID1275491; AID1279234; AID1802457
Mas-related G-protein coupled receptor member X2Homo sapiens (human)EC50 (µMol)15.50000.14003.73818.9000AID1802708; AID1802709
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
sensory perception of painMas-related G-protein coupled receptor member X2Homo sapiens (human)
sleepMas-related G-protein coupled receptor member X2Homo sapiens (human)
positive regulation of cytokinesisMas-related G-protein coupled receptor member X2Homo sapiens (human)
mast cell degranulationMas-related G-protein coupled receptor member X2Homo sapiens (human)
mast cell activationMas-related G-protein coupled receptor member X2Homo sapiens (human)
G protein-coupled receptor signaling pathwayMas-related G-protein coupled receptor member X2Homo sapiens (human)
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)
sensory perception of painMas-related G-protein coupled receptor member X2Homo sapiens (human)
sleepMas-related G-protein coupled receptor member X2Homo sapiens (human)
positive regulation of cytokinesisMas-related G-protein coupled receptor member X2Homo sapiens (human)
mast cell degranulationMas-related G-protein coupled receptor member X2Homo sapiens (human)
mast cell activationMas-related G-protein coupled receptor member X2Homo sapiens (human)
G protein-coupled receptor signaling pathwayMas-related G-protein coupled receptor member X2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityMas-related G-protein coupled receptor member X2Homo sapiens (human)
neuropeptide bindingMas-related G-protein coupled receptor member X2Homo sapiens (human)
mast cell secretagogue receptor activityMas-related G-protein coupled receptor member X2Homo sapiens (human)
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)
G protein-coupled receptor activityMas-related G-protein coupled receptor member X2Homo sapiens (human)
neuropeptide bindingMas-related G-protein coupled receptor member X2Homo sapiens (human)
mast cell secretagogue receptor activityMas-related G-protein coupled receptor member X2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
membraneMas-related G-protein coupled receptor member X2Homo sapiens (human)
plasma membraneMas-related G-protein coupled receptor member X2Homo sapiens (human)
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)
membraneMas-related G-protein coupled receptor member X2Homo sapiens (human)
plasma membraneMas-related G-protein coupled receptor member X2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (70)

Assay IDTitleYearJournalArticle
AID1802709PRESTO-Tango Assay from Article 10.1038/nchembio.2334: \\In silico design of novel probes for the atypical opioid receptor MRGPRX2.\\2017Nature chemical biology, 05, Volume: 13, Issue:5
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
AID1802708Intracellular Calcium Mobilization Assay from Article 10.1038/nchembio.2334: \\In silico design of novel probes for the atypical opioid receptor MRGPRX2.\\2017Nature chemical biology, 05, Volume: 13, Issue:5
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
AID1802457cAMP Inhibition Assay from Article 10.1074/jbc.M113.515668: \\Chemotype-selective modes of action of u00BF-opioid receptor agonists.\\2013The Journal of biological chemistry, Nov-29, Volume: 288, Issue:48
Chemotype-selective modes of action of κ-opioid receptor agonists.
AID1802456Homologous Competition Assay from Article 10.1074/jbc.M113.515668: \\Chemotype-selective modes of action of u00BF-opioid receptor agonists.\\2013The Journal of biological chemistry, Nov-29, Volume: 288, Issue:48
Chemotype-selective modes of action of κ-opioid receptor agonists.
AID65523Effective concentration to inhibit E203Q,D204N,D206N,E209Q KL-2 Opioid receptor kappa 1 binding to [35S]GTP-gamma-S, expressed in COS cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID1773086Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as inhibition of forskolin induced cAMP production by measuring dyn A1-13 Emax incubated with dyn A1-13 alone measured after 30 mins by2021Journal of natural products, 08-27, Volume: 84, Issue:8
Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling.
AID149887Binding affinity to Opioid receptor delta 1 by competitive inhibition of radioligand [3H]DPDPE using cloned receptors transiently expressed on CHO cells1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
AID149830Ratio of potency in the GPI assay (IC50) to Binding affinity (Ki) was determined against Opioid receptor kappa 11997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
AID1773069Agonist activity at mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as beta-arrestin 2 recruitment using furimazine as a substrate preincubated for 5 mins followed by ligand addition measured for 35 mins by BRET assay2021Journal of natural products, 08-27, Volume: 84, Issue:8
Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling.
AID1275491Agonist activity at human recombinant KOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
AID55440Binding constant against D216N,D217N,E218Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID1279234Agonist activity at human recombinant KOR expressed in CHO cells by calcium mobilization assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
AID1279239Intrinsic activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay relative to DPDPE2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
AID148443Effective concentration to inhibit wild type KL-2 Opioid receptor kappa 1 binding to [35S]GTP-gamma-S, expressed in COS cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID331173Ratio of Kcat to Km for ACE22008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Development of potent and selective phosphinic peptide inhibitors of angiotensin-converting enzyme 2.
AID1714329Displacement of [3H]diprenorphine from human MOR expressed in mouse NG108-15 cell membranes incubated for 2 hrs by liquid scintillation counting based radioligand competition assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structure-Activity Relationships of [des-Arg
AID1275483Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis relative to DPDPE2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
AID1714328Displacement of [3H]U69,593 from human KOR expressed in mouse HN9.10 cell membranes incubated for 2 hrs by liquid scintillation counting based radioligand competition assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structure-Activity Relationships of [des-Arg
AID226073Inhibition of [3H]U-69593 binding to kappa opioid receptor of guinea pig brain homogenate1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID1773070Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as binding affinity of dyn A1-13 to orthosteric binding site incubated with dyn A1-13 alone for 90 mins by radioligand competition bind2021Journal of natural products, 08-27, Volume: 84, Issue:8
Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling.
AID1714330Displacement of [3H]deltorphin-II from human DOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting based radioligand competition assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structure-Activity Relationships of [des-Arg
AID148576Binding constant against wild type EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID1773078Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as inhibition of forskolin induced cAMP production by measuring dyn A1-13 EC50 incubated with dyn A1-13 alone measured after 30 mins by2021Journal of natural products, 08-27, Volume: 84, Issue:8
Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling.
AID55438Effective concentration to inhibit D216,ND217N,E218Q KL-2 Opioid receptor kappa 1 binding to [35S]GTP-gamma-S, expressed in COS cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID147934Relative affinity for delta and kappa opioid receptors of guinea pig brain homogenate1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID226072Inhibition of [3H]PL-17 binding to mu opioid receptor of guinea pig brain homogenate1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID148103The compound was tested for binding activity towards opioid receptor kappa in guinea pig brain membranes.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Modification of the enkephalin "message" with an artificial polycationic C-terminus.
AID1279238Intrinsic activity at human recombinant MOR expressed in CHO cells by calcium mobilization assay relative to dermorphin2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
AID1275482Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis relative to EM22016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
AID1279233Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
AID148736Binding affinity towards k-opioid receptor k-EL-2 mutant (wild-type) expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID141262Binding affinity towards Mutant E203Q,D204N,D206N,E209Q Opioid receptor kappa 1 expressed in HEK cells; ND is not determined due to low expression2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID226081Inhibition of delta-selective antagonist binding to opioid receptor of mouse vas dferens1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID141263Binding affinity towards mutant E203Q,D204N,D206N,E209Q Opioid receptor kappa 1 EL-2 expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID149021The compound was tested for binding activity towards opioid receptor mu in guinea pig brain membranes.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Modification of the enkephalin "message" with an artificial polycationic C-terminus.
AID65519Binding constant against E203Q,D204N,D206N EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID749871Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Effect of anchoring 4-anilidopiperidines to opioid peptides.
AID1256748Agonist activity at kappa-opioid receptor (unknown origin) after 90 mins by [35S]GTPgammaS binding assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.
AID141259Binding affinity towards Mutant E203Q,D204N,D206N Opioid receptor kappa 1 expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID150045The compound was tested for binding activity towards Opioid receptor delta 1 in guinea pig brain membranes.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Modification of the enkephalin "message" with an artificial polycationic C-terminus.
AID79195The compound was tested for inhibition of electrically evoked contractions in guinea pig ileum with bestatin at 10e-6 M conc; Not determined1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Modification of the enkephalin "message" with an artificial polycationic C-terminus.
AID65520Effective concentration to inhibit E203Q,D204N,D206N KL-2 Opioid receptor kappa 1 binding to [35S]GTP-gamma-S, expressed in COS cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID65522Binding constant against E203Q,D204N,D206N,E209Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID219259Binding affinity towards Wild-type kappa opioid receptor expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID141519Relative affinity for mu and kappa opioid receptors of guinea pig brain homogenate1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID749876Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Effect of anchoring 4-anilidopiperidines to opioid peptides.
AID141254Binding affinity towards Mutant D216N, D217N, E218Q Opioid receptor kappa 1 expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID1275490Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
AID141261Binding affinity towards Mutant E203Q, D204N, D206N, Opioid receptor kappa 1 EL-2 expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID149847Selectivity for kappa and mu opioid receptors of guinea pig brain and ileum respectively1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID226071Inhibition of [3H]DPDPE binding to delta opioid receptor of guinea pig brain homogenate1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID79187Inhibition of electrically evoked contractions in guinea pig ileum at 10e-6 M conc. with cocktail comprised of 10 uM bestatin, 10 uM captopril, 0.3 uM thiophan, and 10 mM L-leucylleucine; Not determined1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Modification of the enkephalin "message" with an artificial polycationic C-terminus.
AID1275489Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
AID141256Binding affinity towards Mutant D216N, D217N, E218Q Opioid receptor kappa 1 EL-2 expressed in HEK cells2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
AID79040Opioid activity in guinea pig ileum1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
AID749872Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membranes2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Effect of anchoring 4-anilidopiperidines to opioid peptides.
AID226076Inhibition of mu-selective antagonist binding to opioid receptor of guinea pig ileum1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
AID147916Binding affinity to Opioid receptor mu 1 by competitive inhibition of radioligand [3H]DAMGO using cloned receptors transiently expressed on CHO cells1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
AID749873Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membranes2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Effect of anchoring 4-anilidopiperidines to opioid peptides.
AID149137Binding affinity to Opioid receptor kappa 1 by competitive inhibition of radioligand [3H]diprenorphine using cloned receptors transiently expressed on CHO cells1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
AID1279232Agonist activity at human recombinant MOR expressed in CHO cells by calcium mobilization assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
AID149563Ki ratio of compound on Opioid receptor kappa 1, Opioid receptor mu 1, Opioid receptor delta 1 opioid receptor; 1/3/921997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1346411Rat kappa receptor (Opioid receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21
Cloning and pharmacological characterization of a rat kappa opioid receptor.
AID1346329Human kappa 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.
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.
AID1802708Intracellular Calcium Mobilization Assay from Article 10.1038/nchembio.2334: \\In silico design of novel probes for the atypical opioid receptor MRGPRX2.\\2017Nature chemical biology, 05, Volume: 13, Issue:5
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
AID1802709PRESTO-Tango Assay from Article 10.1038/nchembio.2334: \\In silico design of novel probes for the atypical opioid receptor MRGPRX2.\\2017Nature chemical biology, 05, Volume: 13, Issue:5
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,968)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990828 (27.90)18.7374
1990's996 (33.56)18.2507
2000's580 (19.54)29.6817
2010's431 (14.52)24.3611
2020's133 (4.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 49.61

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 Index49.61 (24.57)
Research Supply Index8.05 (2.92)
Research Growth Index4.50 (4.65)
Search Engine Demand Index83.97 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (49.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials24 (0.78%)5.53%
Trials4 (1.09%)5.53%
Reviews213 (6.88%)6.00%
Reviews3 (0.82%)6.00%
Case Studies2 (0.06%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other2,857 (92.28%)84.16%
Other361 (98.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Effects of Dynorphin 1-13 on Heroin Addiction [NCT00000244]Phase 20 participants Interventional1994-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]