Page last updated: 2024-12-05

qx-314

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

Description

QX-314: triethyl analog of lidocaine; RN & NM refer to ion [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3925
CHEMBL ID1180496
CHEBI ID46937
SCHEMBL ID93854
MeSH IDM0059844

Synonyms (51)

Synonym
BRD-K56596464-003-01-8
BRD-K56596464-004-02-4
gtpl2405
[2-[(2,6-dimethylphenyl)amino]-2-oxoethyl]-triethylazanium
tocris-1014
BIO2_000671
NCGC00015612-01
NCGC00024939-01
BIO2_000191
lopac-l-5783
LOPAC0_000679
IDI1_033941
BSPBIO_001471
UPCMLD-DP014:001
UPCMLD-DP014
NCGC00024939-03
NCGC00024939-06
qx-314
CHEBI:46937 ,
NCGC00024939-05
2-[(2,6-dimethylphenyl)amino]-n,n,n-triethyl-2-oxoethanaminium
2-((2,6-dimethylphenyl)amino)-n,n,n-triethyl-2-oxoethanaminium
ethanaminium, 2-((2,6-dimethylphenyl)amino)-n,n,n-triethyl-2-oxo-
qx 314
KBIO2_005327
KBIO3_000381
KBIO3_000382
KBIO2_002759
KBIOSS_000191
KBIO2_000191
KBIOGR_000191
NCGC00024939-04
NCGC00015612-08
CHEMBL1180496
CCG-204765
qx314
46zif6y2x9 ,
unii-46zif6y2x9
NCGC00015612-07
NCGC00015612-04
NCGC00015612-02
NCGC00015612-06
NCGC00015612-05
SCHEMBL93854
DTXSID10943813
Q27088501
triethyl((2,6-xylylcarbamoyl)methyl)ammonium
2-((2,6-dimethylphenyl)amino)-n,n,n-triethyl-2-oxo-ethanaminium
n-ethyllidocaine bromide
NCGC00015612-14
HMS3742C13

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" We also observed animals for electrocardiographic evidence of toxic effects on cardiac automaticity, conductivity, and rhythmicity."( A comparison of the systemic toxicity of lidocaine versus its quaternary derivative QX-314 in mice.
Cheung, HM; Lee, SM; MacLeod, BA; Ries, CR; Schwarz, SK, 2011
)
0.59
" Rats were inspected for durations of effective sensory and motor nerve blocks, systemic adverse effects, and histological changes of local tissues."( The quaternary lidocaine derivative QX-314 in combination with bupivacaine for long-lasting nerve block: Efficacy, toxicity, and the optimal formulation in rats.
Li, J; Liu, J; Lv, R; Ma, L; Yang, X; Yin, Q; Zhang, W; Zheng, Q; Zhu, T, 2017
)
0.73

Compound-Compound Interactions

ExcerptReferenceRelevance
"The quaternary lidocaine derivative (QX-314) in combination with bupivacaine can produce long-lasting nerve blocks in vivo, indicating potential clinical application."( The quaternary lidocaine derivative QX-314 in combination with bupivacaine for long-lasting nerve block: Efficacy, toxicity, and the optimal formulation in rats.
Li, J; Liu, J; Lv, R; Ma, L; Yang, X; Yin, Q; Zhang, W; Zheng, Q; Zhu, T, 2017
)
1

Dosage Studied

ExcerptRelevanceReference
" Both the dose-response curve and the kinetics of the cocaine-induced closures indicate that there is a single class of cocaine-binding site."( Cocaine-induced closures of single batrachotoxin-activated Na+ channels in planar lipid bilayers.
Wang, GK, 1988
)
0.27
" In the presence of higher lidocaine doses, nicotinic receptors were blocked both at positive and negative potentials, acetylcholine dose-response curve shifted to the right and lidocaine pre-application, before its co-application with acetylcholine, enhanced the current inhibition, indicating all together that lidocaine also blocked resting receptors; besides, it increased the current decay rate."( Multiple inhibitory actions of lidocaine on Torpedo nicotinic acetylcholine receptors transplanted to Xenopus oocytes.
Alberola-Die, A; González-Ros, JM; Ivorra, I; Martinez-Pinna, J; Morales, A, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
local anaestheticAny member of a group of drugs that reversibly inhibit the propagation of signals along nerves. Wide variations in potency, stability, toxicity, water-solubility and duration of action determine the route used for administration, e.g. topical, intravenous, epidural or spinal block.
[role 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]

Drug Classes (1)

ClassDescription
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
[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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.63100.100020.879379.4328AID588453
15-lipoxygenase, partialHomo sapiens (human)Potency25.11890.012610.691788.5700AID887
TDP1 proteinHomo sapiens (human)Potency18.35640.000811.382244.6684AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency13.35730.180013.557439.8107AID1460; AID1468
arylsulfatase AHomo sapiens (human)Potency10.69101.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency31.62280.035520.977089.1251AID504332
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency14.21910.00106.000935.4813AID943; AID944
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (28)

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.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347151Optimization of GU AMC 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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346501Mouse Kir3.2 (Inwardly rectifying potassium channels)1996Neuron, May, Volume: 16, Issue:5
Functional analysis of the weaver mutant GIRK2 K+ channel and rescue of weaver granule cells.
AID1864493Substrate activity at human OCT3 overexpressed in HEK293 cells assessed as uptake ratio incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1864501Inhibition of human OCT3 mediated ASP+ uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1864502Inhibition of human OCT3 mediated (S,S)-Ethambutol uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1864503Inhibition of human OCT3 mediated Famotidine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1864505Inhibition of human OCT3 mediated methylscopolamine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1864509Substrate uptake in empty vector transfected (OCT3 null) HEK293 cells incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1864508Substrate uptake at human OCT3 overexpressed in HEK293 cells incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (290)

TimeframeStudies, This Drug (%)All Drugs %
pre-199029 (10.00)18.7374
1990's89 (30.69)18.2507
2000's87 (30.00)29.6817
2010's75 (25.86)24.3611
2020's10 (3.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.11

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 Index32.11 (24.57)
Research Supply Index5.70 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index43.69 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (1.01%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other294 (98.99%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]