Compounds > mavatrep
Page last updated: 2024-11-12

mavatrep

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Description

mavatrep: a transient receptor potential vanilloid 1 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID17751090
CHEMBL ID2364618
SCHEMBL ID1797450
SCHEMBL ID1796599
MeSH IDM000608406

Synonyms (41)

Synonym
unii-f197218t99
trans-2-(2-(2-(2-(4-trifluoromethylphenyl)vinyl)-1h-benzimidazol-5-yl)phenyl)propan-2-ol
f197218t99 ,
jnj-39439335
mavatrep
benzenemethanol, alpha,alpha-dimethyl-2-(2-((1e)-2-(4-(trifluoromethyl)phenyl)ethenyl)-1h-benzimidazol-6-yl)-
jnj 39439335
956274-94-5
mavatrep [usan:inn]
mavatrep (usan)
D10370
benzenemethanol, .alpha.,.alpha.-dimethyl-2-(2-((1e)-2-(4-(trifluoromethyl)phenyl)ethenyl)-1h-benzimidazol-6-yl)-
mavatrep [who-dd]
mavatrep [mi]
mavatrep [usan]
(e)-2-(2-(2-(2-(4-triflouromethyl-phenyl)-vinyl)-1h-benzimidazol-5-yl)-phenyl)-propan-2-ol
mavatrep [inn]
CHEMBL2364618
CS-4591
SCHEMBL1797450
SCHEMBL1796599
AC-33673
HY-16935
bdbm50086717
DTXSID90241905
AKOS030527038
mavatrep(jnj-39439335)
DB12875
(e)-2-(2-(2-(4-(trifluoromethyl)styryl)-1h-benzo[d]imidazol-6-yl)phenyl)propan-2-ol
BCP23936
jnj-39439335; jnj 39439335; jnj39439335
compound 4 [pmid: 25850459]
jnj39439335
gtpl12755
mavatrep; jnj-39439335
EX-A2266
2-[2-[2-[(e)-2-[4-(trifluoromethyl)phenyl]ethenyl]-3h-benzimidazol-5-yl]phenyl]propan-2-ol
Q27277506
A920392
MS-27413
ordhxxhtbuzrcn-nteuormpsa-n

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" All JNJ-39439335-treated participants reported ≥1 treatment-emergent adverse events (TEAE); most common (≥50% incidence) TEAEs in part 1 were feeling hot (79%), thermohypoesthesia (71%), paresthesia (58%) and feeling cold (50%), and in part 2, were minor thermal burns (50%)."( A multiple-dose double-blind randomized study to evaluate the safety, pharmacokinetics, pharmacodynamics and analgesic efficacy of the TRPV1 antagonist JNJ-39439335 (mavatrep).
Flores, CM; Hutchison, JS; Manitpisitkul, P; Mayorga, AJ; Moyer, JA; Romano, G; Shalayda, K; Tatikola, K, 2018)		0.68
" Analgesic efficacy of lower doses administered over a longer period of time and improved patient counseling techniques to reduce the minor thermal burns can be explored to minimize the adverse events."( A multiple-dose double-blind randomized study to evaluate the safety, pharmacokinetics, pharmacodynamics and analgesic efficacy of the TRPV1 antagonist JNJ-39439335 (mavatrep).
Flores, CM; Hutchison, JS; Manitpisitkul, P; Mayorga, AJ; Moyer, JA; Romano, G; Shalayda, K; Tatikola, K, 2018)		0.68

Pharmacokinetics

ExcerptReferenceRelevance
" Marked dose-related increases in pharmacodynamic heat pain assessments were observed in JNJ-39439335-treated participants, which persisted throughout the treatment with no signs of tolerance with repeated dosing."( A multiple-dose double-blind randomized study to evaluate the safety, pharmacokinetics, pharmacodynamics and analgesic efficacy of the TRPV1 antagonist JNJ-39439335 (mavatrep).
Flores, CM; Hutchison, JS; Manitpisitkul, P; Mayorga, AJ; Moyer, JA; Romano, G; Shalayda, K; Tatikola, K, 2018)		0.68
"JNJ-39439335 (doses 2-50 mg) was well-tolerated, and associated with acceptable multiple-dose pharmacokinetic profile."( A multiple-dose double-blind randomized study to evaluate the safety, pharmacokinetics, pharmacodynamics and analgesic efficacy of the TRPV1 antagonist JNJ-39439335 (mavatrep).
Flores, CM; Hutchison, JS; Manitpisitkul, P; Mayorga, AJ; Moyer, JA; Romano, G; Shalayda, K; Tatikola, K, 2018)		0.68

Bioavailability

ExcerptReferenceRelevance
"To improve room temperature stability and oral bioavailability of mavatrep (JNJ-39439335, a transient receptor potential vanilloid subtype-1 antagonist), various formulations were initially developed and evaluated in 2 phase 1 open-label, randomized, 3-way crossover studies in healthy participants."( Bioavailability and Pharmacokinetics of TRPV1 Antagonist Mavatrep (JNJ-39439335) Tablet and Capsule Formulations in Healthy Men: Two Open-Label, Crossover, Single-Dose Phase 1 Studies.
Caruso, J; Manitpisitkul, P; Moyer, JA; Russell, L; Sanga, P; Shalayda, K; Solanki, B; Williams, Y, 2018)		0.96
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)IC50 (µMol)0.02100.00040.21474.0000AID1206377
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)0.00680.00002.015110.0000AID1206379
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)IC50 (µMol)0.01150.00020.606010.0000AID1206358; AID1206378; AID1206379
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Ki0.00650.00010.67956.4000AID1206376
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (53)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
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 (23)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
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 (11)

Processvia Protein(s)Taxonomy
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
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 (57)

Assay IDTitleYearJournalArticle
AID1206371Reversal of complete freund's adjuvant-induced thermal hypersensitivity in po dosed Sprague-Dawley rat measured at 100 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206395Volume of distribution at steady state in mouse at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206404AUC in rat at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206385Reversal of carrageenan-induced thermal hypersensitivity in po dosed Sprague-Dawley rat assessed as plasma concentration required to reach ED50 measured at 100 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206402Cmax in monkey at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206409Half life in monkey at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206364Half life in rat at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206379Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of pH 5-induced current measured for 150 secs by patch clamp assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206366Reversal of complete freund's adjuvant-induced thermal hypersensitivity in Sprague-Dawley rat at 10 mg/kg, po measured after 30 to 180 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206363Clearance in rat at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206401Cmax in dog at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206384Reversal of carrageenan-induced thermal hypersensitivity in po dosed Sprague-Dawley rat measured at 100 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206417Displacement of [3H]-astemizole from recombinant human ERG at 10 uM2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206398Half life in monkey at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206378Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced current measured for 150 secs by patch clamp assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206414Inhibition of CYP3A4 in human liver microsomes2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206397Half life in dog at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206390Clearance in monkey at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206389Clearance in dog at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206413Oral bioavailability in mouse at 10 mg/kg2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206358Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206410Half life in mouse at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206418Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 100 mg/kg, po measured after 0.5 hrs by rectal thermometer relative to vehicle-treated control2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206361Metabolic stability in human liver microsomes assessed as compound remaining after 10 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206411Oral bioavailability in dog at 10 mg/kg2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206405AUC in dog at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206419Toxicity in guinea pig assessed as induction of hemodynamic/electrocardiographic effect at 10 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206377Antagonist activity at recombinant rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206396Half life in rat at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206392Volume of distribution at steady state in rat at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206391Clearance in mouse at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206372Reversal of complete freund's adjuvant-induced thermal hypersensitivity in po dosed Sprague-Dawley rat assessed as plasma concentration required to reach ED50 measured at 100 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206388Metabolic stability in dog liver microsomes assessed as compound remaining after 10 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206394Volume of distribution at steady state in monkey at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206362Oral bioavailability in rat at 10 mg/kg2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206387Metabolic stability in monkey liver microsomes assessed as compound remaining after 10 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206415Inhibition of CYP1A2 in human liver microsomes2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206416Inhibition of CYP2D6 in human liver microsomes2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206407AUC in mouse at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206393Volume of distribution at steady state in dog at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206376Displacement of [3H]-RTX from human TRPV1 transfected in HEK293 cells after 60 mins by scintillation spectroscopic analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206408Half life in dog at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206420Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 100 mg/kg, po measured after 30 to 180 mins by rectal thermometer relative to vehicle-treated control2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206406AUC in monkey at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206360Metabolic stability in rat liver microsomes assessed as compound remaining after 10 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206373Reversal of complete freund's adjuvant-induced thermal hypersensitivity in po dosed Sprague-Dawley rat assessed as plasma concentration required to reach ED80 measured at 100 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206380Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of heat-evoked current at 0.1 uM incubated for 80 secs followed by casazepine treatment measured after 55 secs by patch clamp assay relative to control2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206422Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 10 mg/kg, po qd administered for 5 days measured over 0.5 to 3 hrs post last dose by microchip temperature/ID telemetry probe-based assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206421Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 0.1 to 100 mg/kg, po measured after 0.5 to 5 hrs by microchip temperature/ID telemetry probe-based assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206403Cmax in mouse at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206400Cmax in rat at 10 mg/kg, po2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206412Oral bioavailability in monkey at 10 mg/kg2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206381Effect on TRPM8 (unknown origin)2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206382Effect on TRPV2 (unknown origin)2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206383Effect on TRPA1 (unknown origin)2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206386Reversal of carrageenan-induced thermal hypersensitivity in po dosed Sprague-Dawley rat assessed as plasma concentration required to reach ED80 measured at 100 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID1206399Half life in mouse at 2 mg/kg, iv2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (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: 21.41

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 Index21.41 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (66.67%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other2 (33.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
celecoxib
[no description available]		2.1110organofluorine compound;
pyrazoles;
sulfonamide;
toluenes		cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
naproxen
Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.		3.5311methoxynaphthalene;
monocarboxylic acid		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
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.		3.5611capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
ConditionIndicatedRelationship StrengthStudiesTrials
Allodynia
[description not available]		02.1110
Innate Inflammatory Response
[description not available]		02.1110
Ache
[description not available]		02.1110
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.		02.1110
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		07.1110
Osteoarthritis of Knee
[description not available]		04.5122
Osteoarthritis, Knee
Noninflammatory degenerative disease of the knee joint consisting of three large categories: conditions that block normal synchronous movement, conditions that produce abnormal pathways of motion, and conditions that cause stress concentration resulting in changes to articular cartilage. (Crenshaw, Campbell's Operative Orthopaedics, 8th ed, p2019)		16.5122
Arthritis, Degenerative
[description not available]		02.1510
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.		07.1510
Joint Pain
[description not available]		03.5611
Arthralgia
Pain in the joint.		03.5611