Proteins > Transient receptor potential cation channel subfamily V member 1
Page last updated: 2024-08-07 15:24:21
Transient receptor potential cation channel subfamily V member 1
A transient receptor potential cation channel TRPV1 that is encoded in the genome of rat. [OMA:O35433, PRO:DNx]
Synonyms
TrpV1;
Capsaicin receptor;
Osm-9-like TRP channel 1;
OTRPC1;
Vanilloid receptor 1;
Vanilloid receptor type 1-like
Research
Bioassay Publications (54)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (7.41) | 18.2507 |
| 2000's | 32 (59.26) | 29.6817 |
| 2010's | 15 (27.78) | 24.3611 |
| 2020's | 3 (5.56) | 2.80 |
Compounds (36)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
The SAR analysis of TRPV1 agonists with the α-methylated B-region.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 22, Issue:16, 2012
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond "B-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain "C-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
TRPV1 Modulators for the Treatment of Pain and Inflammation.ACS medicinal chemistry letters, , Feb-14, Volume: 10, Issue:2, 2019
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 20, Issue:23, 2010
Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain "C-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond "B-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 17, Issue:1, 2007
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
The SAR analysis of TRPV1 agonists with the α-methylated B-region.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 22, Issue:16, 2012
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond "B-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 17, Issue:1, 2007
The SAR analysis of TRPV1 agonists with the α-methylated B-region.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 22, Issue:16, 2012
Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain "C-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
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.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Design and synthesis of conformationally restricted capsaicin analogues based in the 1, 3, 4-thiadiazole heterocycle reveal a novel family of transient receptor potential vanilloid 1 (TRPV1) antagonists.European journal of medicinal chemistry, , Volume: 66, 2013
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Silicon switch approach in TRPV1 antagonist MK-056 and its analogues.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists.European journal of medicinal chemistry, , Volume: 44, Issue:1, 2009
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Structure-activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 22, Issue:11, 2012
Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic actiBioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Silicon switch approach in TRPV1 antagonist MK-056 and its analogues.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists.Bioorganic & medicinal chemistry, , Dec-15, Volume: 17, Issue:24, 2009
Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists.Bioorganic & medicinal chemistry, , May-15, Volume: 17, Issue:10, 2009
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.Journal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007