Page last updated: 2024-12-07

ar-c239

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

Description

AR-C239: structure given in first source; alpha(2B)-selective adrenoreceptor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID609483
CHEMBL ID362051
CHEBI ID93630
SCHEMBL ID3944463
MeSH IDM0102577

Synonyms (31)

Synonym
OPREA1_609848
BRD-K93188295-300-01-4
NCGC00024880-01
tocris-0928
arc239
NCGC00024880-02
2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-4,4-dimethyl-(2h,4h)-isoquinoline-1,3-dione
arc 239
2-(2-(4-(o-methoxyphenyl)piperazine-1-yl)ethyl)-4,4-dimethyl-1,3(2h,4h)isoquinolinedione
ar-c239
1,3(2h,4h)-isoquinolinedione, 2-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-4,4-dimethyl-
2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-4,4-dimethylisoquinoline-1,3(2h,4h)-dione
2-{2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl}-4,4-dimethyl-4h-isoquinoline-1,3-dione
bdbm50160151
CHEMBL362051 ,
67339-62-2
unii-m7h349zz5t
m7h349zz5t ,
ar-c-239
SCHEMBL3944463
JFNKXGOEOQCXDM-UHFFFAOYSA-N
1,3(2h,4h)-isoquinolinedione, 2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-4,4-dimethyl-
2-(2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)-4,4-dimethyl-1,3(2h,4h)-isoquinolinedione #
CHEBI:93630
2-[2-[4-(o-methoxyphenyl)piperazin-1-yl]ethyl]4,4-dimethyl-1,3-(2h,4h)isoquinolinedione
Q27165321
DTXSID70986600
2-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-4,4-dimethylisoquinoline-1,3(2h,4h)-dione
CS-0012286
HY-12709
AKOS040747838

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves to 5-bromo-6-(2-imidazoline-2-yl-amino)quinoxaline (UK 14,304) an alpha-2 adrenergic agonist, were generated in the absence and presence of three concentrations of various antagonists."( Alpha-2A and alpha-2B adrenergic receptor subtypes: attenuation of cyclic AMP production in cell lines containing only one receptor subtype.
Bylund, DB; Ray-Prenger, C, 1989
)
0.28
") did not modify the basal activity of the locus coeruleus but shifted to the left the dose-response curve for the clonidine induced inhibition of firing rate and reduced the corresponding ED50 by 77%."( Activation of 5-HT1A receptors potentiates the clonidine inhibitory effect in the locus coeruleus.
Ruiz-Ortega, JA; Ugedo, L, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperazines
[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 (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency24.44930.000811.382244.6684AID686978; AID686979
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926; AID938
regulator of G-protein signaling 4Homo sapiens (human)Potency1.19170.531815.435837.6858AID504845
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.84890.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.84890.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory 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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID239249Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
AID274937Antagonist effect on compound A-induced antinociception in Swiss Albino mouse at 10 mg/kg, ip2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-199011 (25.58)18.7374
1990's16 (37.21)18.2507
2000's10 (23.26)29.6817
2010's4 (9.30)24.3611
2020's2 (4.65)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other45 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]