Page last updated: 2024-11-10

endomorphin 1

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

Description

endomorphin 1: isolated from bovine brain [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311080
CHEMBL ID316446
CHEBI ID177580
MeSH IDM0274734

Synonyms (32)

Synonym
CHEMBL316446 ,
189388-22-5
CHEBI:177580
mfcd01321063
(2s)-1-[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]-n-[(2s)-1-[[(2s)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1h-indol-3-yl)-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
gtpl1623
endomorphin-1 ,
endomorphin 1
NCGC00163676-01
NCGC00163676-02
tyr-pro-trp-phe-nh2
tyrosyl-prolyl-tryptophyl-phenylalaninamide
endomorphin -1
ypwf-nh2
1-[2-amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid [1-(1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-(1h-indol-3-yl)-ethyl]-amide
1-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid [1-((s)-(s)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-(1h-indol-3-yl)-ethyl]-amide
(s)-n-((s)-1-((s)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-3-(1h-indol-3-yl)-1-oxopropan-2-yl)-1-((s)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide
(s)-1-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid [(s)-1-((s)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-(1h-indol-3-yl)-ethyl]-amide
h-tyr-pro-trp-phe-nh2
bdbm50095155
l-phenylalaninamide,l-tyrosyl-l-prolyl-l-tryptophyl-
DTXSID10415505
c34h38n6o5
HB2410
AKOS024456355
l-phenylalaninamide, l-tyrosyl-l-prolyl-l-tryptophyl-
(2s)-2-{[(2s)-1-[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidin-2-yl]formamido}-n-[(1s)-1-carbamoyl-2-phenylethyl]-3-(1h-indol-3-yl)propanamide
HY-P0185
Q4531852
(s)-1-(l-tyrosyl)-n-((s)-1-(((s)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-3-(1h-indol-3-yl)-1-oxopropan-2-yl)pyrrolidine-2-carboxamide
AS-80638
l-tyrosyl-l-prolyl-l-tryptophyl-l-phenylalaninamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" These results suggest that the combination of chemical modification and liposome formulation has great potentials in improving the bioavailability of neuroactive peptides."( In vitro stability and permeability studies of liposomal delivery systems for a novel lipophilic endomorphin 1 analogue.
Blanchfield, JT; Koda, Y; Liang, MT; Toth, I, 2008
)
0.56
"In recent study, in order to improve the bioavailability of endomorphin-1 (EM-1), we designed and synthesized a series of novel EM-1 analogs by replacement of L-Pro(2) by β-Pro, D-Ala or Sar, together with C-terminal oligoarginine-conjugation."( Novel endomorphin-1 analogs with C-terminal oligoarginine-conjugation display systemic antinociceptive activity with less gastrointestinal side effects.
Diao, YX; Gu, N; Qiu, TT; Wang, CL; Zhang, Y, 2015
)
0.42
" However, poor bioavailability and low resistance to enzymatic degradation impede their direct application in the treatment of inflammation."( MEL endomorphins act as potent inflammatory analgesics with the inhibition of activated non-neuronal cells and modulation of pro-inflammatory cytokines.
Cui, JM; Han, CZ; Liu, X; Luo, KY; Ma, MT; Wang, LQ; Wang, R; Wang, Y; Wang, ZJ; Wei, S; Zhang, XH; Zhao, L, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" Endomorphin-1 potentiated viral expression, in a bell-shaped dose-response manner with maximal enhancement approximately equal to 35% at 10(-10) M, in both mixed glial/neuronal cell and purified microglial cell cultures."( Endomorphin-1 potentiates HIV-1 expression in human brain cell cultures: implication of an atypical mu-opioid receptor.
Chao, CC; Gekker, G; Hu, S; Lokensgard, J; Peterson, PK; Portoghese, PS, 1999
)
0.3
" The dose-response curves revealed the development of acute tolerance (tachyphylaxis) to endomorphin."( Antinociceptive effects of intrathecal endomorphin-1 and -2 in rats.
Benedek, G; Horvath, G; Szikszay, M; Tömböly, C, 1999
)
0.3
" Electroacupuncture enhanced the antinociceptive effect of intrathecal endomorphin-1 in the formalin test, resulting in a significant leftward shift in the dose-response curves for intrathecal endomorphin-1 antinociception."( Electroacupuncture potentiates the antinociceptive effect of intrathecal endomorphin-1 in the rat formalin test.
Hao, S; Iwasaki, H; Takahata, O, 2000
)
0.31
") that was inactive against DAMGO, did not affect endomorphin-1-induced antinociception but shifted the dose-response curve of endomorphin-2 3-fold to the right."( Differential antagonism of endomorphin-1 and endomorphin-2 spinal antinociception by naloxonazine and 3-methoxynaltrexone.
Fujimura, T; Hayashi, T; Kastin, AJ; Murayama, K; Sakurada, C; Sakurada, S; Sakurada, T; Takeshita, M; Yonezawa, A; Yuhki, M; Zadina, JE, 2000
)
0.31
" The MOR internalization is dose-dependent, with a similar dose-response to that observed for opioid-induced increases in potassium conductance."( Postsynaptic signaling via the [mu]-opioid receptor: responses of dorsal horn neurons to exogenous opioids and noxious stimulation.
Abbadie, C; Basbaum, AI; Marek, K; Trafton, JA, 2000
)
0.31
" Dose-response curves were determined for endomorphin-1 (0."( The synergistic antinociceptive interactions of endomorphin-1 with dexmedetomidine and/or S(+)-ketamine in rats.
Benedek, G; Dobos, I; Horvath, G; Joo, G; Klimscha, W; Toth, G, 2001
)
0.31
" A 2-h pretreatment with endomorphin-1 (30 nmol) produced a 3-fold shift to the right in the dose-response curve for endomorphin-1."( Acute antinociceptive tolerance and asymmetric cross-tolerance between endomorphin-1 and endomorphin-2 given intracerebroventricularly in the mouse.
Fujimoto, JM; Hung, KC; Mizoguchi, H; Tseng, LF; Wu, HE, 2001
)
0.31
" The failure of naloxone to completely antagonize the effect of the higher concentration of EM-1 or EM-2 could be due to insufficient dosage or might indicate the involvement of non-opiate receptor mechanisms."( Effect of endomorphin on somatostatin secretion in the isolated perfused rat stomach.
Allescher, HD; Lippl, F; Schusdziarra, V,
)
0.13
" and co-administration of 3-methylnaltrexone shifted the dose-response curves for endomorphin-2 induced antinociception to the right by 4-fold."( Differential antagonism of endomorphin-1 and endomorphin-2 supraspinal antinociception by naloxonazine and 3-methylnaltrexone.
Fujimura, T; Hayashi, T; Kastin, AJ; Murayama, K; Sakurada, C; Sakurada, S; Sakurada, T; Sato, T; Takeshita, M; Yonezawa, A; Yuhki, M; Zadina, JE, 2002
)
0.31
" However, injection of nifedipine into the vPAG potentiated the antinociceptive effect of endomorphin-1, producing a significant leftward shift in the dose-response curve of endomorphin-1 in both the tail-flick and tail-pressure tests."( Nifedipine potentiates the antinociceptive effect of endomorphin-1 microinjected into the periaqueductal gray in rats.
Cousins, MJ; Fink, DJ; Hao, S; Iwasaki, H; Mamiya, K; Mata, M; Takahata, O, 2003
)
0.32
" Endomorphin-1, endomorphin-2 and deltorphin I at the dosage of 1, 10, 100 nmol/embryo could stimulate angiogenesis dose-dependently, respectively."( Endogenous opioid peptides, endomorphin-1 and -2 and deltorphin I, stimulate angiogenesis in the CAM assay.
Cui, SG; Dai, X; Liu, Q; Song, HJ; Wang, R; Wang, T, 2008
)
0.35
" In several situations, including clinical depression, MIF-1 exhibits an inverted U-shaped dose-response relationship in which increasing doses can result in decreasing effects."( From MIF-1 to endomorphin: the Tyr-MIF-1 family of peptides.
Kastin, AJ; Pan, W, 2007
)
0.34
" Thus, like given systemically, (+)-morphine given into the posterior nucleus accumbens shell also induces a U-shaped dose-response curve for attenuating the (-)-morphine-produced conditioned place preference."( (+)-Morphine attenuates the (-)-morphine-produced conditioned place preference and the mu-opioid receptor-mediated dopamine increase in the posterior nucleus accumbens of the rat.
Hong, JS; Hung, KC; Schwasinger, ET; Terashvili, M; Tseng, LF; Wu, HE, 2008
)
0.35
" Therefore, coadministration of AEA did not significantly shift the dose-response curve to EM-1."( Antinociceptive interactions between anandamide and endomorphin-1 at the spinal level.
Benedek, G; Horvath, G; Mecs, L; Tuboly, G, 2009
)
0.35
[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 (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency63.09570.004023.8416100.0000AID485290
Microtubule-associated protein tauHomo sapiens (human)Potency0.11220.180013.557439.8107AID1468
DNA polymerase kappa isoform 1Homo sapiens (human)Potency18.88760.031622.3146100.0000AID588579
[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)
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.00110.00011.20929.9700AID408420
Adenosine receptor A1Bos taurus (cattle)Ki0.00110.00000.71316.0000AID408420
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)855.01300.00010.729810.0000AID426389; AID749871
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki4.28470.00000.60689.2330AID1196465; AID1277619; AID149817; AID1667818; AID1807959; AID339692
Mu-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00050.00010.887410.0000AID242329
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00440.00000.38458.6000AID1196464; AID1277617; AID151616; AID151770; AID151771; AID1667817; AID1807958; AID239174; AID339690; AID339691; AID749873
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki6.68420.00000.18683.9500AID148592; AID1667819; AID1807960
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)0.02750.00010.813310.0000AID408424; AID695716; AID695935
Mu-type opioid receptorHomo sapiens (human)Ki0.01580.00000.419710.0000AID1252982; AID148592; AID1917879; AID382893; AID408420; AID449582; AID695711; AID695934; AID698507
Delta-type opioid receptorHomo sapiens (human)Ki2.86850.00000.59789.9300AID1252983; AID148592; AID695712; AID695933; AID698508; AID749872
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki3.71150.00000.20186.4240AID1196466; AID1277618
Kappa-type opioid receptorHomo sapiens (human)Ki2.44120.00000.362410.0000AID148592; AID1872018; AID695713
Mu-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.03630.00081.699210.0000AID151138
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00460.00000.27869.0000AID749873
[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 receptorRattus norvegicus (Norway rat)EC50 (µMol)0.51800.00000.06470.9320AID277680; AID339695
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.02080.00000.32639.4000AID1252985; AID1667820; AID1807965; AID1872048; AID277678; AID698512
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)0.93200.00000.43328.3000AID277680
Mu-type opioid receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.93200.00000.04930.9320AID277680
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (54)

Processvia Protein(s)Taxonomy
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Bos taurus (cattle)
response to purine-containing compoundAdenosine receptor A1Bos taurus (cattle)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (194)

Assay IDTitleYearJournalArticle
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.
AID382897Effect on internalization of mu opioid receptor in HEK293 cells2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.
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.
AID408419Apparent permeability from apical to basolateral side of the human Caco-2 membrane2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID1252985Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID1667818Displacement of [3H]-DPDPE from Wistar rat delta opioid receptor incubated for 3 hrs by liquid scintillation counting method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID1277617Displacement of [3H]DAMGO from rat cortical MOR by liquid scintillation counting method2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
AID239174Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
AID151138Inhibition of Mu opioid receptor of mouse vas deferens2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID695712Displacement of [3H]DPDPE from delta-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID1196472Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology at 3.3 uM measured over 30 mins by label free binding assay relative to DPDPE2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID1456633Selectivity ratio of Ki for displacement of [3H]DPDPE from delta-opioid receptor in Wistar rat membrane to Ki for displacement of [3H]DAMGO from mu-opioid receptor in Wistar rat brain membrane
AID1917879Displacement of [3H]DAMGO from human cloned mu-opioid receptor by radioligand binding assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery.
AID1196466Displacement of [3H]U69,593 from guinea pig cortex/cerebella kappa opioid receptor after 2 hrs by liquid scintillation counting analysis2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID695714Selectivity ratio of Ki for delta-opioid receptor to Ki for mu-opioid receptor2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID698512Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1562920Displacement of [3H]JWH-018 from CB1R/CB2R in Wistar rat brain membranes at 10 uM after 60 mins by liquid scintillation analysis2019European journal of medicinal chemistry, Sep-15, Volume: 178Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors.
AID1807976Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv measured after 20 mins by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID408418Metabolic stability assessed as half life in human Caco-2 cell homogenate2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID382893Displacement of [3H]DAMGO from mu opioid receptor in human SH-SY5Y cells2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.
AID149817Displacement of [3H]Ile5,6-deltorphin II from opioid receptor delta 1 of rat brain membranes2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID1807964Inhibition of electric-field induced mouse vas deferens contraction2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID398178Stability in rat brain homogenates assessed as degradation half life2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.
AID1277621Selectivity ratio of Ki for rat cortical DOR to Ki for rat cortical MOR2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
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.
AID151432Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.
AID295477Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
AID1456636Half life in Kunming mouse brain homogenate at 500 uM by RP-HPLC method
AID695713Displacement of [3H]diprenorphine from kappa-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID339696Half life in rat brain membrane homogenate2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
AID695936Selectivity ratio of Ki for DOP receptor expressed in CHO-K1 cells to Ki for MOP receptor expressed in CHO-K1 cells2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.
AID1277620Selectivity ratio of Ki for guinea pig KOR to Ki for rat cortical MOR2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
AID151616Binding affinity towards Opioid receptor mu 12000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.
AID698513Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction in presence of delta opioid receptor antagonist naltrindole2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID277678Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
AID1252982Displacement of [3H]-DAMGO from mu opioid receptor (unknown origin) transfected in HEK293 cells2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID408417Displacement of [3H]DAMGO from delta opioid receptor in rat brain membrane2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID339692Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
AID293121Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked muscle contractions2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
AID339693Selectivity ratio of Ki for displacement of [3H]DAMGO from mu opioid receptor over Ki for displacement of [3H]Ile5,6deltorphin from delta opioid receptor in Wistar rat brain2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
AID1253002Antinociceptive activity in mouse assessed as inhibition of tail flick at 4 mg/kg, iv measured at 5 to 60 mins2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID1252984Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for mu opioid receptor (unknown origin)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID695707Apparent permeability across human Caco2 cells at 200 uM by LC/MS analysis2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID151447Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance.
AID698516Agonist activity at human FLAG-tagged mu opioid receptor expressed in HEK293 cells assessed as induction of ERK1/2 phosphorylation after 10 mins by Western blot analysis2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID408424Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID587666Agonist activity at opioid receptor in mu rat brain membrane by [35S]GTPgammaS binding assay relative to baseline in presence of opioid-selective antagonist naloxone2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
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.
AID1371090Displacement of [3H]-DPDPE from delta opioid receptor in Wistar rat brain membranes preincubated for 3 hrs measured after 1 hr by scintillation counting method2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Original endomorphin-1 analogues exhibit good analgesic effects.
AID1807965Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID195718In vitro effective dose against [35S]GTP-gamma-S, binding to rat brain membranes2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID698510Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1196467Selectivity ratio of Ki for rat cortex delta opioid receptor to Ki for rat cortex mu opioid receptor2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID1249927Displacement of [3H]diprenorphine from zebrafish delta1b opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
AID1807960Displacement of [3H]-U69593 from KOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID698520Half life in mouse brain homogenates2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1249925Displacement of [3H]diprenorphine from zebrafish mu opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
AID339690Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
AID1667822Half life in Kunming mouse brain homogenate at 10'-2 mol/L by RP-HPLC analysis2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID698511Selectivity ratio of IC50 for mu opioid receptor in guinea pig ileum to IC50 for delta opioid receptor in Kunming mouse vas deferens2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID587667Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay relative to baseline2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
AID1277618Displacement of [3H]U69,593 from guinea pig KOR after 2 hrs by liquid scintillation counting method2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
AID1872050Stability in mouse brain homogenate assessed as half life2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1456637Half life in Kunming mouse plasma at 500 uM by RP-HPLC method
AID277682Agonist activity at mu opioid receptor by inhibition of electrically evoked muscle contraction in guinea pig ileum2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
AID408421Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID295478Selectivity for rat mu opioid receptor over rat delta opioid2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
AID408422Selectivity for rat mu opioid receptor over rat delta opioid receptor2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID587664Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
AID242329Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
AID1277619Displacement of [3H]DPDPE from rat cortical DOR after 2.5 hrs by liquid scintillation counting method2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
AID587665Half life in rat brain homogenate by RP-HPLC2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
AID587662Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane homogenate by liquid scintillation counting2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
AID1252999Antinociceptive activity in mouse prolonged tonic phase inflammatory pain model assessed as inhibition of formalin-induced licking/biting behavior at 4 mg/kg, iv2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID277684Agonist activity at delta opioid receptor by inhibition of electrically evoked muscle contraction in isolated mouse vas deferens2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
AID1807970Metabolic stability in Kunming mouse serum assessed as half life measured upto 480 mins by RP-HPLC analysis2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1075901Half life in human plasma by RP-HPLC analysis2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Delivery of a lactose derivative of endomorphin 1 to the brain via the olfactory epithelial pathway.
AID426389Agonist activity at delta opioid receptor in mouse vas deference assessed as inhibition of electrically-stimulated contraction2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
AID1807972Antinociceptive activity in icv dosed Kunming mouse model assessed as increase in paw withdrawal latency by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1807963Inhibition of electric-field induced guinea pig ileum contraction2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID295476Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
AID151770Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID1808010Chronic antinociceptive tolerance in Kunming mouse pretreated with compound followed by repeated compound addition at 20 nmol, icv once daily for 7 days and measured after 5 mins by radiant heat paw withdrawal test2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID231320Relative affinity for delta and kappa opioid receptors2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID1667820Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID1808004Tolerance ratio of ED50 for Kunming mouse pretreated with 3 times ED50 of compound for 2 hrs followed by challenge with second dose of compound to ED50 for Kunming mouse pretreated with saline for 2 hrs followed by compound addition2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1807974Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv measured after 5 mins by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID426387Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane by liquid scintillation counting2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
AID1249928Selectivity index, ratio of Ki for zebrafish delta1a opioid receptor to Ki for zebrafish mu opioid receptor2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
AID277680Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
AID195849In vitro percent maximal stimulation of [35S]GTP-gamma-S, binding by the compound in rat brain membranes2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID1667824Antinociceptive activity in kunming mouse models assessed as inhibition of tail-flick response by tail-flick assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID293117Displacement of [3H]deltorphin 2 from delta opioid receptor in rat brain P2 synaptosome2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
AID587663Selectivity ratio of Ki for delta opioid receptor in rat brain to mu opioid receptor in rat brain2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
AID695715Selectivity ratio of Ki for kappa-opioid receptor to Ki for mu-opioid receptor2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID1252998Antinociceptive activity in mouse acute phase inflammatory pain model assessed as inhibition of formalin-induced licking/biting behavior at 4 mg/kg, iv2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID1808003Antinociceptive tolerance in Kunming mouse pretreated with 3 times ED50 of compound for 2 hrs followed by challenge with second dose of compound by radiant heat paw withdrawal test2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1807980Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 20 mins with naloxonazine followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1196465Displacement of [3H]DPDPE from rat cortex delta opioid receptor after 2.5 hrs by liquid scintillation counting analysis2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID695722Antinociceptive activity in Sprague-Dawley rat chronic constriction injury model assessed as paw withdrawal threshold to von Frey filament-induced pain 16 umol/kg, iv administered as bolus injection measured at 15 mins2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID398174Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membrane2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.
AID12705Half-life in rat brain homogenate2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID1667819Displacement of[3H]-U69,593 from Wistar rat kappa opioid receptor incubated for 1.5 hrs by liquid scintillation counting method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID1807973Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID698508Displacement of [3H]DPDPE from Myc-tagged delta opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1371089Displacement of [3H]-DAMGO from mu opioid receptor in Wistar rat brain membranes preincubated for 1 hr measured after 1hr by scintillation counting method2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Original endomorphin-1 analogues exhibit good analgesic effects.
AID151771Displacement of [3H]endomorphin-2 from Opioid receptor mu 1 of rat brain membranes2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID1872052Stability in rat plasma assessed as half life2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1807982Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 30 mins with nor-BNI followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1252989Antinociceptive activity in mouse assessed as inhibition of tail flick at 2 to 20 nmol, icv measured after 30 mins2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID1252986Antinociceptive activity in icv dosed mouse assessed as inhibition of tail flick measured at 5 to 60 mins2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID1807983Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 10 micromol/kg, sc by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID751788Antiallodynic activity in Sprague-Dawley rat chronic constriction injury model assessed as change in ipsilateral hindpaw withdrawal threshold at 0.16 to 16 umol/kg, iv administered as single bolus dose separated by 2 to 3 days wash-out period2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Peripherally acting novel lipo-endomorphin-1 peptides in neuropathic pain without producing constipation.
AID1807978Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 10 mins with naloxone followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID695711Displacement of [3H]DAMGO from mu-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID293116Displacement of [3H]DAMGO from mu opioid receptor in rat brain P2 synaptosome2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
AID339695Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
AID1667834Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method relative to control2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID1196471Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as change in cell morphology at 3.3 uM measured over 30 mins by label free binding assay relative to DAMGO2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID1196475Half life in rat brain homogenate at 10 uM2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID1252988Antinociceptive activity in mouse assessed as inhibition of tail flick at 2 to 20 nmol, icv measured up to 30 mins relative to control2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID587661Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane homogenate by liquid scintillation counting2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
AID1807971Octanol/buffer distribution coefficient, log D of the compound at pH 7.4 by RP-HPLC analysis2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID698507Displacement of [3H]DAMGO from FLAG-tagged mu opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID277689Antinociceptive activity in Swiss Albino mouse assessed as effect on paw licking by hot plate method at 10 ug2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
AID149744Inhibition of Opioid receptor mu 1 of guinea pig ileum2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID695935Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.
AID398173Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membrane2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.
AID1872018Displacement of [3H]U69593 from KOP (unknown origin) stably expressed in HEK293 cells by liquid scintillation counter analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1807961Selectivity index, ratio of Ki for displacement of [3H]DPDPE from DOR in Wistar rat brain membranes to Ki for displacement of [3H]DAMGO from MOR in Wistar rat brain membranes2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID148592Displacement of [3H]dynorphin A from Opioid receptor kappa 1 of rat brain membranes (DAMGO/DADLE quenching of mu/delta receptor binding)2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID1371095Antinociceptive activity in Kunming mouse assessed as increase in latency to withdrawal by measuring AUC at 10 mg/kg, sc measured up to 45 mins post dose by tail-flick test2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Original endomorphin-1 analogues exhibit good analgesic effects.
AID1808013Toxicity in icv dosed Kunming mouse assessed as inhibition of gastrointestinal transit by measuring charcoal distance travel by charcoal meal test2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1872048Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulation2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID398175Selectivity ratio of IC50 for delta opioid receptor to IC50 for mu opioid receptor in Wistar rat brain membrane2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.
AID1456659Antinociceptive activity in mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal at 10 nmol/kg, icv measured up to 60 mins by tail flick test
AID1667825Antinociceptive activity in kunming mouse models assessed as maximum possible effect at 0.4 nmol, icv measured from 5 to 60 mins by warm water tail-flick assay relative to control2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID339694Selectivity ratio of Ki for displacement of [3H]endomorphin-2 from mu opioid receptor over Ki for displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
AID1807962Selectivity index, ratio of Ki for displacement of [3H]-U69593 from KOR in Wistar rat brain membranes to Ki for displacement of [3H]DAMGO from MOR in Wistar rat brain membranes2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID698515Agonist activity at human FLAG-tagged mu opioid receptor expressed in HEK293 cells assessed as induction of ERK1/2 phosphorylation at 10 nM after 10 mins by Western blot analysis2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID695716Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID449582Binding affinity to human mu opioid receptor2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.
AID1371091Selectivity ratio of Ki from delta opioid receptor in Wistar rat brain membranes to Ki from mu opioid receptor in Wistar rat brain membranes2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Original endomorphin-1 analogues exhibit good analgesic effects.
AID1667828Antinociceptive activity in kunming mouse models assessed as effective dose after icv administration measured from 5 to 60 mins by warm water tail-flick assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID698514Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter relative to control2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1872049Stability in mouse serum assessed as half life2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1371093Half life in Kunming mouse plasma at 500 uM by RP-HPLC analysis2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Original endomorphin-1 analogues exhibit good analgesic effects.
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.
AID226741Relative inhibition of mu opioid receptor of guinea pig ileum and mouse vas deferens2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID408423Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production at 100 nM2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID1667836Antinociceptive activity in kunming mouse models assessed as maximum possible effect at 4 nmol, icv measured from 5 to 60 mins by warm water tail-flick assay relative to control2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID1456634Displacement of [3H]DAMGO from mu-opioid receptor in Wistar rat brain membrane after 1 hr by microbeta scintillation counting method
AID293118Selectivity for rat mu opioid receptor over rat delta opioid receptor2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
AID426390Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
AID695938Apparent permeability across human Caco2 cells st 200 uM measured over 150 mins by LC/MS analysis2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.
AID698509Selectivity ratio of Ki for Myc-tagged delta opioid receptor to Ki for FLAG-tagged mu opioid receptor2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID695933Displacement of [3H]DPDPE from DOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.
AID698506Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1667823Half life in Kunming mouse serum at 10'-2 mol/L by RP-HPLC analysis2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID277691Antinociceptive activity in Swiss Albino mouse assessed as effect on jumping by hot plate method at 10 ug2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
AID1807979Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 4 hrs with beta-FNA followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID695934Displacement of [3H]DAMGO from MOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.
AID1667817Displacement of [3H]-DAMGO from Wistar rat mu opioid receptor incubated for 1 hr by liquid scintillation counting method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
AID277690Antinociceptive activity in Swiss Albino mouse assessed as effect on rearing by hot plate method at 10 ug2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
AID1872053Stability in human plasma assessed as half life2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1196468Selectivity ratio of Ki for guinea pig cortex/cerebella kappa opioid receptor to Ki for rat cortex mu opioid receptor2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID1456635Displacement of [3H]DPDPE from delta-opioid receptor in Wistar rat brain membrane after 3 hrs by microbeta scintillation counting method
AID1808002Antinociceptive tolerance in Kunming mouse pretreated with saline for 2 hrs followed by compound addition by radiant heat paw withdrawal test2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1252983Displacement of [3H]-DPDPE from delta opioid receptor (unknown origin) transfected in HEK293 cells2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
AID339691Displacement of [3H]endomorphin-2 from mu opioid receptor in Wistar rat brain2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
AID698517Agonist activity at human FLAG-tagged mu opioid receptor expressed in HEK293 cells assessed as induction of ERK1/2 phosphorylation at 1 pM after 10 mins by Western blot analysis2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1807969Metabolic stability in Kunming mouse brain assessed as half life measured upto 480 mins by RP-HPLC analysis2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1808015Toxicity in Kunming mouse model assessed as conditioned place preference time at 20 nmol, icv2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1196464Displacement of [3H]DAMGO from rat cortex mu opioid receptor after 30 mins by liquid scintillation counting analysis2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
AID201473Potency for inhibition of forskolin-stimulated cyclic AMP accumulation in SH-SY5Y cells2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance.
AID1808014Toxicity in Kunming mouse assessed as inhibition of gastrointestinal transit at 10 micromol/kg, sc by charcoal meal test (Rvb = 70.3 +/- 3 %)2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1808016Toxicity in Kunming mouse model assessed as conditioned place preference time at 10 micromol/kg, sc2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1807959Displacement of [3H]DPDPE from DOR in Wistar rat brain membranes measured after 3 hrs by scintillation counting method2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID293119Agonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of electrically evoked myenteric plexus longitudinal muscle contractions2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
AID695937Half life in human Caco2 cell homogenate at 200 uM by LC/MS analysis2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.
AID1371094Antinociceptive activity in Kunming mouse assessed as increase in latency to withdrawal by measuring AUC at 20 nmol/kg, i.c.v measured up to 45 mins post dose by tail-flick test2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Original endomorphin-1 analogues exhibit good analgesic effects.
AID695706Half life in human plasma at 1 mg/ml by RP-HPLC analysis2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID151468Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance.
AID408420Displacement of [3H]DAMGO from mu opioid receptor in human SHSY5Y cells2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
AID1807958Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1807966Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA relative to control2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
AID1371092Half life in Kunming mouse 15% brain homogenate at 500 uM by RP-HPLC analysis2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
Original endomorphin-1 analogues exhibit good analgesic effects.
AID695718Plasma concentration in Sprague-Dawley rat at 10 umol/kg, po from 30 to 60 mins by LC/MS analysis2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
AID1249926Displacement of [3H]diprenorphine from zebrafish delta1a opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
AID698518Antinociceptive activity in icv dosed Kunming mouse assessed as inhibition of heat-induced tail flick after 5 to 60 mins2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).
AID1346364Human mu receptor (Opioid receptors)1997Nature, Apr-03, Volume: 386, Issue:6624
A potent and selective endogenous agonist for the mu-opiate receptor.
AID1346361Human delta receptor (Opioid receptors)1998FEBS letters, Nov-13, Volume: 439, Issue:1-2
Endomorphins fully activate a cloned human mu opioid receptor.
AID1346364Human mu receptor (Opioid receptors)1998FEBS letters, Nov-13, Volume: 439, Issue:1-2
Endomorphins fully activate a cloned human mu opioid receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (442)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's62 (14.03)18.2507
2000's256 (57.92)29.6817
2010's104 (23.53)24.3611
2020's20 (4.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.86

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

MetricThis Compound (vs All)
Research Demand Index21.86 (24.57)
Research Supply Index6.11 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (0.45%)5.53%
Reviews29 (6.47%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other417 (93.08%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]