Compounds > abt 116
Page last updated: 2024-11-13

abt 116

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Description

ABT 116: a TRPV1 antagonist with analgesic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46890602
CHEMBL ID1085324
SCHEMBL ID3104060
MeSH IDM0548863

Synonyms (15)

Synonym
CHEMBL1085324 ,
1-(2-(3,3-dimethylbutyl)-4-(trifluoromethyl)benzyl)-3-(1-methyl-1h-indazol-4-yl)urea
bdbm50319454
abt 116
urea, n-((2-(3,3-dimethylbutyl)-4-(trifluoromethyl)phenyl)methyl)-n'-(1-methyl-1h-indazol-4-yl)-
1008529-42-7
unii-373jc9fj2h
373jc9fj2h ,
abt-116
SCHEMBL3104060
urea, n-[[2-(3,3-dimethylbutyl)-4-(trifluoromethyl)phenyl]methyl]-n'-(1-methyl-1h-indazol-4-yl)-
DTXSID80143545
1-[2-(3,3-dimethylbutyl)-4-(trifluoromethyl) benzyl]-3-(1-methyl-1h-indazol-4-yl)urea
Q27256622
AKOS040750031
[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)0.27700.00040.21474.0000AID483346
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)IC50 (µMol)0.01100.00020.606010.0000AID483345; AID483353
[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 (18)

Assay IDTitleYearJournalArticle
AID483341Oral bioavailability in rat at 10 mg/kg2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483333Antiinflammatory activity against carrageenan-induced thermal hyperalgesia in po dosed rat2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483337Volume of distribution at steady state in rat at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483351Solubility in lipid2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483350Antiinflammatory activity in rat osteoarthritis model assessed as reduction of pain in rat at 10 umol/kg, po bid measured after 12 days2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483346Antagonist activity at rat TRPV1 assessed as inhibition of capsaicin-induced effect2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483349Antiinflammatory activity in rat post operative pain model assessed as reduction in pain in rat at 100 umol/kg, po measured after 12 days2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483338Plasma clearance in rat at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483335Aqueous solubility of the compound2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483340Half life in rat at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483348Inhibition of CYP3A4 assessed as midazolam oxidation at 10 uM2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483353Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of N-arachidonoyl-dopamine-induced effect2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483352Toxicity in rat assessed as increase of body temperature at 100 umol/kg, po after 1 hr2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483354Antiinflammatory activity in rat osteoarthritis model assessed as reduction of pain in rat at 10 umol/kg, po measured after 12 days2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483345Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced effect at pH 5.52010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483339Cmax in rat at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483342Ratio of drug level in brain to plasma in rat at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
AID483334Antiinflammatory activity in rat osteoarthritis model assessed as inhibition of thermal hyperalgesia in po dosed rat2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Discovery of TRPV1 antagonist ABT-116.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (100.00)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: 12.88

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 Index12.88 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (60.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other2 (40.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
uric acid
Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.		3.4611uric acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
carprofen
carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs.		3.4611carbazoles;
organochlorine compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug;
photosensitizing agent
4-butyrolactone
4-Butyrolactone: One of the FURANS with a carbonyl thereby forming a cyclic lactone. It is an endogenous compound made from gamma-aminobutyrate and is the precursor of gamma-hydroxybutyrate. It is also used as a pharmacological agent and solvent.. tetrahydrofuranone : Any oxolane having an oxo- substituent at any position on the tetrahydrofuran ring.. gamma-butyrolactone : A butan-4-olide that is tetrahydrofuran substituted by an oxo group at position 2.		3.4611butan-4-olidemetabolite;
neurotoxin
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		5.4853indazole
tramadol
Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.. tramadol : A racemate consisting of equal amounts of (R,R)- and (S,S)-tramadol. A centrally acting synthetic opioid analgesic, used (as the hydrochloride salt) to treat moderately severe pain. The (R,R)-enantiomer exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. Originally developed by Gruenenthal GmbH and launched in 1977, it was subsequently isolated from the root bark of the South African tree Nauclea latifolia.. (R,R)-tramadol : A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.		3.46112-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanoladrenergic uptake inhibitor;
antitussive;
capsaicin receptor antagonist;
delta-opioid receptor agonist;
kappa-opioid receptor agonist;
metabolite;
mu-opioid receptor agonist;
muscarinic antagonist;
nicotinic antagonist;
NMDA receptor antagonist;
opioid analgesic;
serotonergic antagonist;
serotonin uptake inhibitor
firocoxib
firocoxib: a COX-2 inhibitor; structure in first source. firocoxib : An enol ether that is the cyclopropylmethyl ether of 3-hydroxy-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]furan-2-one. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in horses and dogs.		3.4611butenolide;
cyclopropanes;
enol ether;
sulfone		antineoplastic agent;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
buprenorphine
Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain.		3.4611morphinane alkaloiddelta-opioid receptor antagonist;
kappa-opioid receptor antagonist;
mu-opioid receptor agonist;
opioid analgesic
abt 102
ABT 102: a TRPV1 antagonist; structure in first source		2.0510
ConditionIndicatedRelationship StrengthStudiesTrials
Canine Diseases
[description not available]		04.4222
Plica Syndrome
[description not available]		03.4611
Gait Disorders, Animal
[description not available]		04.4222
Synovitis
Inflammation of the SYNOVIAL MEMBRANE.		03.4611
Ache
[description not available]		04.4222
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		04.4222
Coxarthrosis
[description not available]		03.4611
Osteoarthritis, Hip
Noninflammatory degenerative disease of the hip joint which usually appears in late middle or old age. It is characterized by growth or maturational disturbances in the femoral neck and head, as well as acetabular dysplasia. A dominant symptom is pain on weight-bearing or motion.		03.4611