Page last updated: 2024-11-12

neuromedin u 8

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

Cross-References

ID SourceID
PubMed CID10351235
CHEMBL ID3356083
SCHEMBL ID8808129
MeSH IDM0134142

Synonyms (8)

Synonym
SCHEMBL8808129
neuromedin u 8(swinespinal cord)(9ci)
bdbm50049425
CHEMBL3356083 ,
neuromedin u-8 (porcine)
(2s)-2-[[(2s)-2-[[(2s)-1-[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-
CS-0656308
HY-P4763

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"4% at 30 nmol/kg) by once-daily repeated dosing for 2 weeks in mice with diet-induced obesity."( Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
Asakawa, T; Asami, T; Dote, K; Fujita, H; Hirabayashi, H; Inooka, H; Kaisho, T; Kanematsu-Yamaki, Y; Matsumiya, K; Mochida, T; Nagai, H; Nishizawa, N; Ohtaki, T; Sakamoto, J; Takekawa, S, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuromedin-U receptor 2Homo sapiens (human)IC50 (µMol)0.00170.00170.00170.0017AID1352039; AID1355077
Neuromedin-U receptor 1Homo sapiens (human)IC50 (µMol)0.00080.00080.00080.0008AID1352038; AID1355076
[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)
Neuromedin-U receptor 1Mus musculus (house mouse)EC50 (µMol)0.00360.00060.00360.0095AID1182312; AID1446045; AID1464658
Neuromedin-U receptor 2Mus musculus (house mouse)EC50 (µMol)0.00120.00020.00120.0030AID1182313; AID1446046; AID1464659
Neuromedin-U receptor 2Homo sapiens (human)EC50 (µMol)0.01560.00041.31046.6000AID1352034; AID1355079; AID1446044; AID1464657
Neuromedin-U receptor 1Homo sapiens (human)EC50 (µMol)0.01970.00040.01970.0389AID1352032; AID1355078; AID1446043; AID1464656
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
reduction of food intake in response to dietary excessNeuromedin-U receptor 2Homo sapiens (human)
regulation of smooth muscle contractionNeuromedin-U receptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeuromedin-U receptor 2Homo sapiens (human)
neuropeptide signaling pathwayNeuromedin-U receptor 2Homo sapiens (human)
cell-cell signalingNeuromedin-U receptor 2Homo sapiens (human)
central nervous system developmentNeuromedin-U receptor 2Homo sapiens (human)
grooming behaviorNeuromedin-U receptor 2Homo sapiens (human)
feeding behaviorNeuromedin-U receptor 2Homo sapiens (human)
response to painNeuromedin-U receptor 2Homo sapiens (human)
arachidonic acid secretionNeuromedin-U receptor 2Homo sapiens (human)
positive regulation of calcium-mediated signalingNeuromedin-U receptor 2Homo sapiens (human)
chloride transmembrane transportNeuromedin-U receptor 2Homo sapiens (human)
chloride transportNeuromedin-U receptor 1Homo sapiens (human)
smooth muscle contractionNeuromedin-U receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuromedin-U receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeuromedin-U receptor 1Homo sapiens (human)
neuropeptide signaling pathwayNeuromedin-U receptor 1Homo sapiens (human)
calcium-mediated signalingNeuromedin-U receptor 1Homo sapiens (human)
positive regulation of calcium-mediated signalingNeuromedin-U receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
neuromedin U receptor activityNeuromedin-U receptor 2Homo sapiens (human)
G protein-coupled receptor activityNeuromedin-U receptor 2Homo sapiens (human)
intracellularly calcium-gated chloride channel activityNeuromedin-U receptor 2Homo sapiens (human)
protein bindingNeuromedin-U receptor 2Homo sapiens (human)
GTP bindingNeuromedin-U receptor 2Homo sapiens (human)
neuromedin U bindingNeuromedin-U receptor 2Homo sapiens (human)
neuropeptide receptor activityNeuromedin-U receptor 2Homo sapiens (human)
neuromedin U receptor activityNeuromedin-U receptor 1Homo sapiens (human)
G protein-coupled receptor activityNeuromedin-U receptor 1Homo sapiens (human)
neuromedin U bindingNeuromedin-U receptor 1Homo sapiens (human)
neuropeptide receptor activityNeuromedin-U receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneNeuromedin-U receptor 2Homo sapiens (human)
membraneNeuromedin-U receptor 2Homo sapiens (human)
plasma membraneNeuromedin-U receptor 2Homo sapiens (human)
plasma membraneNeuromedin-U receptor 1Homo sapiens (human)
membraneNeuromedin-U receptor 1Homo sapiens (human)
plasma membraneNeuromedin-U receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID1352034Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of potent and proteolytically stable human neuromedin U receptor agonists.
AID1464659Agonist activity at mouse NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
A potent neuromedin U receptor 2-selective alkylated peptide.
AID1355083Half life in human plasma by LC-UV-MS analysis2018ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5
Synthesis and
AID1352039Displacement of [3H]-NMU-8 from human NMUR2 expressed in HEK293 cell membranes after 3 hrs by microscintillation counting2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of potent and proteolytically stable human neuromedin U receptor agonists.
AID1355079Agonist activity at human NMUR2 expressed in HEK293 cells assessed as IP3 accumulation after 60 mins in presence of myo-[2-3H(N)]inositol by scintillation proximity assay2018ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5
Synthesis and
AID1446045Agonist activity at mouse NMUR1 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
AID1352041Half life in human plasma at 112 uM by HPLC-UV/MS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of potent and proteolytically stable human neuromedin U receptor agonists.
AID1355081Selectivity ratio of IC50 for human NMUR2 expressed in HEK293 to IC50 for human NMUR1 expressed in HEK293 cells2018ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5
Synthesis and
AID1355078Agonist activity at human NMUR1 expressed in HEK293 cells assessed as IP3 accumulation after 60 mins in presence of myo-[2-3H(N)]inositol by scintillation proximity assay2018ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5
Synthesis and
AID1464658Agonist activity at mouse NMUR1 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
A potent neuromedin U receptor 2-selective alkylated peptide.
AID1352040Selectivity ratio of IC50 for human NMUR2 expressed in HEK293 cell membranes to IC50 for NMUR1 expressed in HEK293 cell membranes2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of potent and proteolytically stable human neuromedin U receptor agonists.
AID1355076Displacement of [3H]-NMU-8 from human NMUR1 expressed in HEK293 cells after 3 hrs by topcount micro scintillation counting method2018ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5
Synthesis and
AID1446044Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
AID1182312Agonist activity at mouse NMUR1 expressed in HEK293 cells by calcium mobilization assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of selective hexapeptide agonists to human neuromedin U receptors types 1 and 2.
AID1464657Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
A potent neuromedin U receptor 2-selective alkylated peptide.
AID1446043Agonist activity at human NMUR1 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
AID1355077Displacement of [3H]-NMU-8 from human NMUR2 expressed in HEK293 cells after 3 hrs by topcount micro scintillation counting method2018ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5
Synthesis and
AID1182313Agonist activity at mouse NMUR2 expressed in HEK293 cells by calcium mobilization assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of selective hexapeptide agonists to human neuromedin U receptors types 1 and 2.
AID1352032Agonist activity at human NMUR1 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of potent and proteolytically stable human neuromedin U receptor agonists.
AID1464656Agonist activity at human NMUR1 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
A potent neuromedin U receptor 2-selective alkylated peptide.
AID1446046Agonist activity at mouse NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
AID1352038Displacement of [3H]-NMU-8 from human NMUR1 expressed in HEK293 cell membranes after 3 hrs by microscintillation counting2018European journal of medicinal chemistry, Jan-20, Volume: 144Development of potent and proteolytically stable human neuromedin U receptor agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.72

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

MetricThis Compound (vs All)
Research Demand Index12.72 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]