Page last updated: 2024-11-07

bdp 12

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

Description

1-(quinoxalin-6-ylcarbonyl)piperidine: modulates AMPA receptor desensitization ; an analog of 1-(1,3-benzodioxol-5-ylcarbonyl)piperidine [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID148184
CHEMBL ID136800
CHEBI ID34605
SCHEMBL ID194605
MeSH IDM0256028

Synonyms (54)

Synonym
AC-001 ,
6-(piperidine-1-carbonyl)quinoxaline
cx516
bdp 12
1-(6-quinoxalinylcarbonyl)piperidine
1-(quinoxalin-6-ylcarbonyl)piperidine
piperidine, 1-(6-quinoxalinylcarbonyl)-
cx 516
1-piperidinyl-6-quinoxalinyl-methanone
154235-83-3
ampalex
cx-516
bdbm50094009
piperidin-1-yl-quinoxalin-6-yl-methanone
chebi:34605 ,
CHEMBL136800 ,
VU0430675-1
spd-420
piperidin-1-yl(quinoxalin-6-yl)methanone
bdp-12
FT-0657266
unii-z5qu38b4v9
z5qu38b4v9 ,
BCP9000296
CX5 ,
HY-10933
CS-1086
BCP0726000046
AKOS008927689
1-piperidinyl-6-quinoxalinylmethanone
FS-3368
1-(quinoxalin-6-ylcarbonyl)-piperidine
gtpl4165
6-[(piperidin-1-yl)carbonyl]quinoxaline
ANDGGVOPIJEHOF-UHFFFAOYSA-N
SCHEMBL194605
1-piperidyl(quinoxalin-6-yl)methanone
DS-1548
DTXSID70165574
ampalex i(1/4)oecx-516
mfcd00943201
EX-A265
ampakine cx516
cx516, >=98% (hplc)
J-009084
NCGC00371146-01
173047-75-1
bdp-12(ampalex)
BCP04606
Q5014875
DB06247
ampalex (cx-516)
AMY14816
ampalex, cx-516

Research Excerpts

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

Dosage Studied

ExcerptRelevanceReference
" More importantly, even millimolar concentrations of CX516 did not influence the dose-response relation for CX546, suggesting the possibility that they bind to different sites."( Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action.
Arai, AC; Kessler, M; Lynch, G; Rogers, G; Xia, YF, 2002
)
0.31
" Problems with potency of CX516 in other studies have suggested dosing may have been inadequate for therapeutic effect and thus it remains unclear whether modulation of AMPA-mediated neurotransmission is a viable therapeutic strategy for the treatment of FXS."( Effect of CX516, an AMPA-modulating compound, on cognition and behavior in fragile X syndrome: a controlled trial.
Berry-Kravis, E; Block, SS; Cogswell, J; Cook, E; Decle, P; Guter, S; Hagerman, R; Jardini, T; Johnson, SA; Krause, SE; Lara, R; Leurgans, S; Maino, D; Potanos, K; Salt, J; Weinberg, D; Wuu, J, 2006
)
0.33
" 30 min prior to the acquisition trial of the NOR task animals were dosed with either vehicle, CX546 (10, 40 or 80 mg/kg) or CX516 (0."( Positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors reverses sub-chronic PCP-induced deficits in the novel object recognition task in rats.
Damgaard, T; Grayson, B; Hansen, SL; Larsen, DB; Neill, JC; Plath, N, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
N-acylpiperidine
[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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)IC50 (µMol)0.10000.00220.57502.7000AID1918507
[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)
Glutamate receptor 4Homo sapiens (human)EC50 (µMol)718.66670.29002.87727.6000AID223222; AID536772
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
kidney development15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
prostaglandin metabolic process15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
transforming growth factor beta receptor signaling pathway15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
female pregnancy15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
parturition15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
lipoxygenase pathway15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
ovulation15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
response to estradiol15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
response to lipopolysaccharide15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
positive regulation of apoptotic process15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
response to ethanol15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
negative regulation of cell cycle15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
thrombin-activated receptor signaling pathway15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
ductus arteriosus closure15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
regulation of prostaglandin catabolic process15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 4Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic processGlutamate receptor 4Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 4Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
prostaglandin E receptor activity15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
oxidoreductase activity, acting on the CH-OH group of donors, NAD or NADP as acceptor15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
identical protein binding15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
NAD binding15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
NAD+ binding15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 4Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 4Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
nucleoplasm15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
cytosol15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
basolateral plasma membrane15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
extracellular exosome15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
cytoplasm15-hydroxyprostaglandin dehydrogenase [NAD(+)]Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendriteGlutamate receptor 4Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 4Homo sapiens (human)
neuronal cell bodyGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
extracellular vesicleGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 4Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 4Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID536772Inhibition of GluR4 expressed in HEK293 cells2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
AID1918507Inhibition of 15-PGDH (unknown origin) using NAD as substrate measured for 3.5 mins2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Orally Bioavailable Quinoxaline Inhibitors of 15-Prostaglandin Dehydrogenase (15-PGDH) Promote Tissue Repair and Regeneration.
AID536770Inhibition of GluR3/4 rat in hippocampal neuron2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
AID223222Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.
AID536771Agonist activity at rat AMPA receptor assessed as change in EPSC amplitude2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (59)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's13 (22.03)18.2507
2000's30 (50.85)29.6817
2010's11 (18.64)24.3611
2020's5 (8.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.89

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 Index22.89 (24.57)
Research Supply Index4.25 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index24.28 (26.88)
Search Engine Supply Index2.67 (0.95)

This Compound (22.89)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (11.29%)5.53%
Reviews8 (12.90%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other47 (75.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]