Compounds > 1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea
Page last updated: 2024-11-11

1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea

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Description

1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID8068410
CHEMBL ID104028
SCHEMBL ID2730561
MeSH IDM0488382

Synonyms (35)

Synonym
bdbm20334
jmc48744 compound 14a
1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea
chembl104028 ,
1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]methyl}urea
a-425619
A831772
581809-67-8
1-(5-isoquinolinyl)-3-[[4-(trifluoromethyl)phenyl]methyl]urea
1-isoquinolin-5-yl-3-[[4-(trifluoromethyl)phenyl]methyl]urea
1-(4-(trifluoromethyl)benzyl)-3-(isoquinolin-5-yl)urea
a- 25619
unii-n2noa4ce04
1-isoquinolin-5-yl-3-(4-(trifluoromethyl)benzyl)urea
urea, n-5-isoquinolinyl-n'-((4-(trifluoromethyl)phenyl)methyl)-
n2noa4ce04 ,
urea, n-5-isoquinolinyl-n'-[[4-(trifluoromethyl)phenyl]methyl]-
gtpl4117
a425619
a 425619
3-(isoquinolin-5-yl)-1-{[4-(trifluoromethyl)phenyl]methyl}urea
SCHEMBL2730561
n-isoquinolin-5-yl-n'-[4-(trifluoromethyl)benzyl]urea
DTXSID20206906
Z164679900
n-5-isoquinolinyl-n'-[[(4-(trifluoromethyl)phenyl]methyl]urea
AKOS027470287
1-(isoquinolin-5-yl)-3-(4-(trifluoromethyl)benzyl)urea
1-(5-isoquinolyl)-3-[[4-(trifluoromethyl)phenyl]methyl]urea
Q27074071
CS-0033160
1-(isoquinolin-5-yl)-3-{[4-(trifluoromethyl)phenyl]methyl}urea
EN300-1266074
urea,n-5-isoquinolinyl-n'-[[4-(trifluoromethyl)phenyl]methyl]-
HY-110292

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharmacokinetic properties."( Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Bayburt, EK; Didomenico, S; Drizin, I; Faltynek, CR; Gomtsyan, A; Honore, P; Jinkerson, TK; Keddy, R; Koenig, JR; Lee, CH; Marsh, KC; McDonald, HA; Mikusa, J; Perner, RJ; Surowy, CS; Turner, SC; Wetter, JM, 2007)		0.34

Bioavailability

ExcerptReferenceRelevance
" The 5-isoquinoline-containing compound 14a (hTRPV1 IC50 = 4 nM) exhibited 46% oral bioavailability and in vivo activity in animal models of visceral and inflammatory pain."( Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Bayburt, EK; Didomenico, S; Drizin, I; Faltynek, CR; Gomtsyan, A; Hannick, SM; Honore, P; Jarvis, MF; Jinkerson, T; Koenig, JR; Lee, CH; Macri, BS; Marsh, KC; McDonald, HA; Oie, T; Perner, RJ; Schmidt, RG; Stewart, KD; Surowy, CS; Turner, S; Wetter, J; Wismer, CT; Zheng, GZ, 2005)		0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)IC50 (µMol)0.01650.00040.21474.0000AID242241; AID313140
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)IC50 (µMol)0.00350.00020.606010.0000AID218474; AID241296; AID290826; AID291897; AID312825; AID313138; AID313139; AID578615
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Ki0.02340.00010.67956.4000AID1190831; AID1797976; AID218483
[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)
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)EC50 (µMol)0.01400.00050.43182.3800AID1797973
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)EC50 (µMol)0.00850.00051.06746.3096AID1797969; AID1797972; AID1797973
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
thermoceptionTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IITransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
fever generationTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
microglial cell activationTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
diet induced thermogenesisTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
peptide secretionTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
negative regulation of systemic arterial blood pressureTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
lipid metabolic processTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cell surface receptor signaling pathwayTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
chemosensory behaviorTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
negative regulation of heart rateTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
negative regulation of mitochondrial membrane potentialTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
glutamate secretionTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
calcium-mediated signalingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cellular response to heatTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
positive regulation of apoptotic processTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
response to peptide hormoneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
behavioral response to painTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
sensory perception of mechanical stimulusTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
detection of temperature stimulus involved in thermoceptionTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
protein homotetramerizationTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
excitatory postsynaptic potentialTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
smooth muscle contraction involved in micturitionTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cellular response to alkaloidTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cellular response to ATPTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cellular response to tumor necrosis factorTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cellular response to acidic pHTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cellular response to temperature stimulusTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
negative regulation of establishment of blood-brain barrierTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
calcium ion import across plasma membraneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
response to capsazepineTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
cellular response to nerve growth factor stimulusTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
transmembrane signaling receptor activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
extracellular ligand-gated monoatomic ion channel activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
voltage-gated calcium channel activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
calcium channel activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
protein bindingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
calmodulin bindingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
ATP bindingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
intracellularly gated calcium channel activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
chloride channel regulator activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
phosphatidylinositol bindingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
identical protein bindingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
metal ion bindingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
phosphoprotein bindingTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
temperature-gated ion channel activityTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
plasma membraneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
external side of plasma membraneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
membraneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
dendritic spine membraneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
neuronal cell bodyTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
postsynaptic membraneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily V member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1797973Ca2+ Influx Functional Assay for the Determination of in Vitro Activity. from Article 10.1021/jm0492958: \\Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinol2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID1797976Radioligand Binding Assay and Antagonist Ca2+ Influx Functional Assay from Article 10.1124/jpet.107.124305: \\[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand2007The Journal of pharmacology and experimental therapeutics, Oct, Volume: 323, Issue:1
[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
AID1797969Ca2+ Influx Functional Assay for the Determination of in Vitro Activity. from Article 10.1021/jm070276i: \\In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 an2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
AID1797972Ca2+ Influx Functional Assay for the Determination of in Vitro Activity. from Article 10.1016/j.bmcl.2007.04.105: \\Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and highe2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID290829Volume of distribution in rat at 10 umol/kg, iv2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID290826Antagonist activity at human TRPV1 by calcium influx assay2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID313139Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
AID247019Concentration required to reduce thermal hyperalgesia in the complete Freund's adjuvant (CFA) model of chronic inflammatory pain2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID1640019Luciferase/luciferin-expressing antifolate-resistant parasites were used to infect a culture of HepG2 cells that were pre-incubated with compounds. Infected hepatocytes emit light due to the luciferase reaction. Assay results are presented as the percent 2018Science (New York, N.Y.), 12-07, Volume: 362, Issue:6419
Open-source discovery of chemical leads for next-generation chemoprotective antimalarials.
AID1190831Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced effect by FLIPR assay2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.
AID244448Plasma protein binding in human2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID291897Antagonist activity at human TRPV1 receptor by calcium influx assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
AID313140Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
AID290828Half life in dog at 10 umol/kg, iv2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID237454Volume of distribution in rat2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID218483Binding affinity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane using [3H]-RTX as radioligand.2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.
AID578615Antagonist activity at human TRPV1 assessed as inhibition of calcium influx2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.
AID290827Half life in rat at 10 umol/kg, iv2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID313144Oral bioavailability in rat2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
AID241296Inhibition of binding to human vanilloid receptor subtype VR12005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID236925Half life in rat2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID290831Plasma clearance in rat at 10 umol/kg, iv2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID1640018Luciferase/luciferin-expressing antifolate-resistant parasites were used to infect a culture of HepG2 cells that were pre-incubated with compounds. Infected hepatocytes emit light due to the luciferase reaction. Assay results are presented as the percent 2018Science (New York, N.Y.), 12-07, Volume: 362, Issue:6419
Open-source discovery of chemical leads for next-generation chemoprotective antimalarials.
AID290834Bioavailability in dog at 10 umol/kg, po2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID244447Plasma protein binding in rat2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID290832Plasma clearance in dog at 10 umol/kg, iv2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID218474Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [Ca2+] levels.2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.
AID291899Stability in human liver microsomes at 0.5 uM after 30 mins2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
AID312825Blockade of human TRPV1 receptor assessed as inhibition of capsaicin-induced calcium flux2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.
AID291898Stability in rat liver microsomes at 0.5 uM after 30 mins2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
AID313138Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
AID236607Maximum concentration in rat2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID290830Volume of distribution in dog at 10 umol/kg, iv2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID290833Bioavailability in rat at 10 umol/kg, po2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
AID242241Inhibition of binding to rat transient receptor potential vanilloid 1 receptor2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
AID1346617Human TRPV1 (Transient Receptor Potential channels)2005The Journal of pharmacology and experimental therapeutics, Jul, Volume: 314, Issue:1
A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (66.67)29.6817
2010's7 (33.33)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: 11.22

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 Index11.22 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.22)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (95.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.520amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
formaldehyde
paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy		2.0210aldehyde;
one-carbon compound		allergen;
carcinogenic agent;
disinfectant;
EC 3.5.1.4 (amidase) inhibitor;
environmental contaminant;
Escherichia coli metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		3.84110isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
acridone
acridone : A member of the class of acridines that is 9,10-dihydroacridine substituted by an oxo group at position 9.		2.1710acridines;
cyclic ketone
ethacridine
Ethacridine: A topically applied anti-infective agent.		2.1710acridines
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		2.17101-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
ym 58483
[no description available]		2.1710
camphor, (+-)-isomer
[no description available]		2.1710bornane monoterpenoid;
cyclic monoterpene ketone		plant metabolite
carbonyl cyanide m-chlorophenyl hydrazone
Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.		2.1710hydrazone;
monochlorobenzenes;
nitrile		antibacterial agent;
geroprotector;
ionophore
carbonyl cyanide p-trifluoromethoxyphenylhydrazone
Carbonyl Cyanide p-Trifluoromethoxyphenylhydrazone: A proton ionophore that is commonly used as an uncoupling agent in biochemical studies.. carbonyl cyanide p-trifluoromethoxyphenylhydrazone : A hydrazone that is hydrazonomalononitrile in which one of the hydrazine hydrogens is substituted by a p-trifluoromethoxyphenyl group.		2.1710aromatic ether;
hydrazone;
nitrile;
organofluorine compound		ATP synthase inhibitor;
geroprotector;
ionophore
papaverine
Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum.		2.1710benzylisoquinoline alkaloid;
dimethoxybenzene;
isoquinolines		antispasmodic drug;
vasodilator agent
pimobendan
pimobendan: produces arterial & venous dilatation in dogs; structure given in first source		2.1710benzimidazoles;
pyridazinone		cardiotonic drug;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		2.1710diarylmethane
n-isopropyl-n-phenyl-4-phenylenediamine
N-isopropyl-N'-phenyl-p-phenylenediamine : The N-substituted diamine that is 1,4-phenylenediamine substituted at one N with an isopropyl group and at the other with a phenyl group.		2.1710N-substituted diamineallergen;
antioxidant
3-amino-9-ethylcarbazole
3-amino-9-ethylcarbazole: RN given refers to parent cpd		2.1710carbazoles
cycloguanil
cycloguanil: the active metabolite of proguanil; antifolate drug; structure in first source. cycloguanil : A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil.		2.1710triazinesantifolate;
antiinfective agent;
antimalarial;
antiparasitic agent;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
2,4,6-trichlorophenyl 4-nitrophenyl ether
2,4,6-trichlorophenyl 4-nitrophenyl ether: structure		2.1710aromatic ether;
C-nitro compound;
chlorobenzenes		EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide
2-phenylthiazolidine-4-carboxylic acid
2-phenylthiazolidine-4-carboxylic acid: RN given refers to cpd without isomeric designation		2.1710
benz(cd)indol-2(1h)-one
benz(cd)indol-2(1H)-one: structure in first source		2.1710
tetraphenylcyclopentadienone
tetraphenylcyclopentadienone: singlet oxygen trapping agent		2.1710stilbenoid
3-(2-pyridyl)-5,6-diphenyl-1,2,4-triazine
[no description available]		2.17101,2,4-triazines
honokiol
[no description available]		2.1710biphenyls
bathophenanthroline
4,7-diphenyl-1,10-phenanthroline : A member of the class of phenanthrolines that is 1,10-phenanthroline bearing two phenyl substituents at positions 4 and 7.		2.1710benzenes;
phenanthrolines		chelator
2-phenyl-4,5-dichloro-3-pyridazinone
[no description available]		2.1710
n-benzylmaleimide
[no description available]		2.1710
phenylglycine nitrile
phenylglycine nitrile: structure in first source		2.1710
4,5-dimethyl-1,2-phenylenediamine
4,5-dimethyl-1,2-phenylenediamine: RN given refers to parent cpd		2.1710
mmv665852
MMV665852: an antischistosomal agent		2.1710
n-(2-methoxyphenyl)maleimide
N-(2-methoxyphenyl)maleimide: structure given in first source		2.1710
2-aminoperimidine
2-aminoperimidine: inhibits bacterial NhaA Na/H+ antiporters; structure in first source		2.1710
1,3-bis(3-chlorophenyl)urea
[no description available]		2.1710ureas
2-phenyl-4-oxohydroquinoline
2-phenyl-4-oxohydroquinoline: structure given in first source		2.1710
2-chloro-3-(4-methylanilino)naphthalene-1,4-dione
[no description available]		2.17101,4-naphthoquinones
mequindox
Mequindox: a synthetic quinoxaline 1,4-dioxide derivative which can effectively improve growth and feed efficiency in animals; structure in first source		2.1710
1,3-bis(3,5-dichlorophenyl)urea
1,3-bis(3,5-dichlorophenyl)urea: COH - City of Hope; has antineoplastic activity		2.1710
dienestrol
Dienestrol: A synthetic, non-steroidal estrogen structurally related to stilbestrol. It is used, usually as the cream, in the treatment of menopausal and postmenopausal symptoms.. dienestrol : An olefinic compound that is hexa-2,4-diene substituted by 4-hydroxyphenyl groups at positions 3 and 4 respectively.		2.1710
(e)-3-(4-t-butylphenyl)-n-(2,3-dihydrobenzo(b)(1,4)dioxin-6-yl)acrylamide
3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo(b)(1,4)dioxin-6-yl)acrylamide: a vanilloid receptor 1 antagonist and antihyperalgesic agent; structure in first source		3.1310
cinnamoylglycine
cinnamoylglycine: structure given in first source. N-cinnamoylglycine : An N-acylglycine in which the acyl group is specified as (2E)-3-phenylprop-2-enoyl (cinnamoyl).		2.1710N-acylglycinemetabolite
4-(4-ethoxyphenyl)-4-oxobutanoic acid
[no description available]		2.1710aromatic ketone
3-(4-chlorophenyl)-5-propyl-1H-pyrazolo[1,5-a]pyrimidin-7-one
[no description available]		2.1710pyrazoles;
ring assembly
N-[4-[methyl(phenyl)sulfamoyl]phenyl]-2-thiophenecarboxamide
[no description available]		2.1710aromatic amide
4-chloro-N-[3-cyano-4-(phenylthio)phenyl]benzamide
[no description available]		2.1710benzamides
3-(4-morpholinyl)-4-(2-pyridinyl)-N-[3-(trifluoromethyl)phenyl]-1-pyrazolecarboxamide
[no description available]		2.1710pyrazolopyridine
capsaicin
ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.		3.5580capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
7-chloro-2-methyl-4-(4-methylphenyl)sulfonylthiazolo[5,4-b]indole
[no description available]		2.1710sulfonamide
4-[2-[(2,6-dimethoxyphenyl)-oxomethoxy]-1-oxoethyl]-2,5-dimethyl-1H-pyrrole-3-carboxylic acid ethyl ester
[no description available]		2.1710methoxybenzoic acid
2-(1H-benzimidazol-2-ylthio)-1-(2,5-dimethyl-1-prop-2-enyl-3-pyrrolyl)ethanone
[no description available]		2.1710benzimidazoles
2,3-dihydro-1,4-dioxin-5-carboxylic acid [2-[4-[4-(2-methylbutan-2-yl)phenoxy]anilino]-2-oxoethyl] ester
[no description available]		2.1710aromatic ether
2-(1,3-benzoxazol-2-ylthio)-1-(2,5-dimethyl-1-prop-2-enyl-3-pyrrolyl)ethanone
[no description available]		2.1710benzoxazole
capsazepine
capsazepine: modified capsaicin molecule; a capsaicin receptor antagonist. capsazepine : A benzazepine that is 2,3,4,5-tetrahydro-1H-2-benzazepine which is substituted by hydroxy groups at positions 7 and 8 and on the nitrogen atom by a 2-(p-chlorophenyl)ethylaminothiocarbonyl group. A synthetic analogue of capsaicin, it was the first reported capsaicin receptor antagonist.		3.8230benzazepine;
catechols;
monochlorobenzenes;
thioureas		capsaicin receptor antagonist
3-(4-chlorophenyl)-2-methyl-3,3a,4,5-tetrahydrobenzo[g]indazole
[no description available]		2.1710tetralins
6-hydroxy-4-methyl-2-phenyl-2,3-dihydropyridazin-3-one
[no description available]		2.1710pyridazinone
1-(4-chlorophenyl)-3-[4-methyl-2-(thiophen-2-yl)-1,3-thiazol-5-yl]urea
1-(4-chlorophenyl)-3-[4-methyl-2-(thiophen-2-yl)-1,3-thiazol-5-yl]urea : An member of the class of phenylureas that is urea having 4-chlorophenyl and 4-methyl-2-(thiophen-2-yl)-1,3-thiazol-5-yl groups attached at positions 1 and 3 respectively.		2.17101,3-thiazoles;
monochlorobenzenes;
phenylureas;
thiophenes
N'-[(4-chlorophenyl)-oxomethyl]-2-methyl-4-thiazolecarbohydrazide
[no description available]		2.1710carbonyl compound;
organohalogen compound
bi-78d3
[no description available]		2.1710aryl sulfide
n-(3-chloro-4-methylphenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide
N-(3-chloro-4-methylphenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide: activates the plant defense response; structure in first source. tiadinil : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid with the amino group of 3-chloro-4-methylaniline. It is a fungicide used particularly for the control of fungal diseases in rice.		2.1710anilide fungicide;
monocarboxylic acid amide;
monochlorobenzenes;
organosulfur compound;
thiadiazoles		antifungal agrochemical
N'2-[3-(trifluoromethyl)benzoyl]-3-aminopyrazine-2-carbohydrazide
[no description available]		2.1710(trifluoromethyl)benzenes
2-amino-4-(2-chlorophenyl)-6-[(4-chlorophenyl)thio]pyridine-3,5-dicarbonitrile
[no description available]		2.1710phenylpyridine
2-[5-[(3-chlorophenyl)thio]-2-thiophenyl]pyridine
[no description available]		2.1710aryl sulfide
8-methylsulfinyl-4,5-dihydrothieno[3,4-g][2,1]benzoxazole-6-carboxylic acid ethyl ester
[no description available]		2.1710thiophenecarboxylic acid
1-(5-tert-butyl-2-methyl-3-pyrazolyl)-3-(3,5-dichlorophenyl)urea
[no description available]		2.1710ureas
4-[[4-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-7-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-2-yl]methyl]morpholine
[no description available]		2.1710isoquinolines
7-chloro-3-hydroxy-2-[3-(trifluoromethyl)phenyl]-4-quinazolinone
[no description available]		2.1710quinazolines
2-(1H-benzimidazol-2-ylthio)-1-[2,5-dimethyl-1-(2-oxolanylmethyl)-3-pyrrolyl]ethanone
[no description available]		2.1710benzimidazoles
ethyl 4-(3-oxo-2,3-dihydroisothiazol-2-yl)benzoate
[no description available]		2.1710organic molecular entity
7-chloro-N-(phenylmethyl)-4-quinolinamine
[no description available]		2.1710aminoquinoline
6-methoxy-2-methyl-N-[[3-(trifluoromethyl)phenyl]methyl]-4-quinolinamine
[no description available]		2.1710aminoquinoline
arachidonyl dopamine
arachidonyl dopamine: a ligand for the vanilloid receptor VR1		2.0310catechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide
olvanil
[no description available]		2.0310methoxybenzenes;
phenols
2-acetylpyridine thiosemicarbazone
2-acetylpyridine thiosemicarbazone: RN given refers to parent cpd		2.1710
sanshool
sanshool: isolated from the stem bark of Zanthoxylum liebmannianum; RN given for (E,E,Z,E)-isomer; structure in first source		2.0510fatty amide
4-(4-chlorophenyl)-3-methylbut-3-en-2-oxime
4-(4-chlorophenyl)-3-methylbut-3-en-2-oxime: a TRPA1 antagonist		2.1710
n-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2h)-carboxamide
N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide: a vanilloid receptor 1 antagonist and analgesic; structure in first source		3.1310piperazines;
pyridines
abt 102
ABT 102: a TRPV1 antagonist; structure in first source		2.0410
jnj 17203212
[no description available]		3.1310
a 784168
1-(3-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethylsulfonyl)phenyl)-1,2,3,6-tetrahydropyridine-4-carboxamide: a TRPV1 antagonist		2.0310
a 803467
A 803467: an Nav1.8 sodium channel blocker; structure in first source		2.0510
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.1650
Allodynia
[description not available]		02.9540
Ache
[description not available]		04.3470
Colicky Pain
[description not available]		02.0210
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		09.3470
Abdominal Pain
Sensation of discomfort, distress, or agony in the abdominal region.		02.0210
Innate Inflammatory Response
[description not available]		02.9740
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		07.9740
Infections, Plasmodium
[description not available]		02.1710
Malaria
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.		02.1710
Joint Pain
[description not available]		02.1710
Arthralgia
Pain in the joint.		02.1710
Pyrexia
[description not available]		02.0410
Hypothermia, Accidental
[description not available]		02.0410
Fever
An abnormal elevation of body temperature, usually as a result of a pathologic process.		02.0410
Hypothermia
Lower than normal body temperature, especially in warm-blooded animals.		02.0410
Chemical Dependence
[description not available]		02.0510
Substance-Related Disorders
Disorders related to substance use or abuse.		02.0510
Nerve Pain
[description not available]		02.0510
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.0510
Dysesthesia
[description not available]		02.0510
HbS Disease
[description not available]		02.0610
Anoxemia
[description not available]		02.0610
Anemia, Sickle Cell
A disease characterized by chronic hemolytic anemia, episodic painful crises, and pathologic involvement of many organs. It is the clinical expression of homozygosity for hemoglobin S.		02.0610
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		02.0610
Chronic Illness
[description not available]		02.0210
Anasarca
[description not available]		02.0210
Arthritis, Degenerative
[description not available]		02.0210
Acute Post-operative Pain
[description not available]		02.0210
Acute Disease
Disease having a short and relatively severe course.		02.0210
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		02.0210
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		02.0210
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		02.0210
Pain, Postoperative
Pain during the period after surgery.		02.0210