Page last updated: 2024-11-12

act 058362

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

Description

1-(2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl)-3-(2-methylquinolin-4-yl)urea: a urotensin-II receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10173280
CHEMBL ID567303
SCHEMBL ID1363480
MeSH IDM0476151

Synonyms (31)

Synonym
act-058362
urea, n-(2-(4-hydroxy-4-(phenylmethyl)-1-piperidinyl)ethyl)-n'-(2-methyl-4-quinolinyl)-
palosuran
1-(2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl-3-(2-methylquinolin-4-yl)urea
1-(2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl)-3-(2-methylquinolin-4-yl)urea
CHEMBL567303 ,
bdbm50302272
uld9zke457 ,
unii-uld9zke457
540769-28-6
palosuran [inn]
gtpl3516
1-[2-[4-hydroxy-4-(phenylmethyl)piperidin-1-yl]ethyl]-3-(2-methylquinolin-4-yl)urea
HY-10655
CS-1722
SCHEMBL1363480
1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea
WYJCYXOCHXWTHG-UHFFFAOYSA-N
AC-35242
DTXSID00202406
AKOS026750332
1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
mfcd07772352
NCGC00408890-01
act 058362
act058362 (palosuran)
BCP15786
Q27088242
act 058362; palosuran
MS-27325
A917972

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The apparent terminal elimination half-life was approximately 20 hours."( Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects.
Dingemanse, J; Sidharta, PN; van Giersbergen, PL, 2009
)
0.35

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency8.48660.00108.379861.1304AID1645840
[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)
Urotensin-2 receptorRattus norvegicus (Norway rat)IC50 (µMol)75.00000.03403.16687.6000AID445487
Urotensin-2 receptorHomo sapiens (human)IC50 (µMol)0.12130.00500.05720.3200AID445489; AID741599; AID741600
Urotensin-2 receptorHomo sapiens (human)Ki0.04100.00080.67724.0000AID445488
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
signal transductionUrotensin-2 receptorHomo sapiens (human)
blood circulationUrotensin-2 receptorHomo sapiens (human)
regulation of blood pressureUrotensin-2 receptorHomo sapiens (human)
blood vessel diameter maintenanceUrotensin-2 receptorHomo sapiens (human)
neuropeptide signaling pathwayUrotensin-2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityUrotensin-2 receptorHomo sapiens (human)
urotensin II receptor activityUrotensin-2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneUrotensin-2 receptorHomo sapiens (human)
membraneUrotensin-2 receptorHomo sapiens (human)
plasma membraneUrotensin-2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine 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.
AID741599Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis2013Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.
AID741600Displacement of [125I]-U2 from recombinant human urotensin2 receptor expressed in human U2OS cells after 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.
AID445487Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.
AID445489Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.
AID445488Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.
AID741610Drug metabolism in human liver microsomes relative to total liver blood flow2013Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.
AID1346328Human UT receptor (Urotensin receptor)2004The Journal of pharmacology and experimental therapeutics, Oct, Volume: 311, Issue:1
Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (36)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's17 (47.22)29.6817
2010's16 (44.44)24.3611
2020's3 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.64

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 Index10.64 (24.57)
Research Supply Index3.81 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.64)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (15.79%)5.53%
Reviews4 (10.53%)6.00%
Case Studies1 (2.63%)4.05%
Observational0 (0.00%)0.25%
Other27 (71.05%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]