88 articles for thisTarget
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Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain"C-region".
Sandoz Institute For Medical Research
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond"B-region".
Sandoz Institute For Medical Research
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.
Seoul National University
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.
Seoul National University
Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists.
Sookmyung Women'S University
Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.
Seoul National University
Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects.
Seoul National University
Partial Activation and Inhibition of TRPV1 Channels by Evodiamine and Rutaecarpine, Two Major Components of the Fruits of Evodia rutaecarpa.
TBA
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).
TBA
a-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists.
Seoul National University
The carbonate analogues of 5'-halogenated resiniferatoxin as TRPV1 ligands.
Seoul National University
The SAR analysis of TRPV1 agonists with thea-methylated B-region.
Seoul National University
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.
Seoul National University
Structure-activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism.
Seoul National University
Receptor activity and conformational analysis of 5'-halogenated resiniferatoxin analogs as TRPV1 ligands.
Seoul National University
Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Ferrara University
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
Neurogen
Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists.
Seoul National University
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Amgen
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
Amgen
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.
Universidad Complutense
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.
Universidad Complutense
Synthesis and evaluation of phorboid 20-homovanillates: discovery of a class of ligands binding to the vanilloid (capsaicin) receptor with different degrees of cooperativity.
Institute
Similarities and differences in the structure-activity relationships of capsaicin and resiniferatoxin analogues.
Institute For Medical Research
3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists.
Seoul National University
2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the B and C-regions.
Shenyang Pharmaceutical University
Triazine-based vanilloid 1 receptor open channel blockers: design, synthesis, evaluation, and SAR analysis.
Institut De Qu£Mica Avan£Ada De Catalunya
Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence.
Bayer Yakuhin
1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties.
Johnson & Johnson Pharmaceutical Research and Development
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Seoul National University
Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites.
Neurogen
Silicon switch approach in TRPV1 antagonist MK-056 and its analogues.
Sookmyung Women'S University
Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists.
Seoul National University
Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists.
Seoul National University
Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
National Institute of Diabetes and Digestive and Kidney Diseases
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Glaxosmithkline
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
Abbott Laboratories
Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
Neurogen
Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists.
Seoul National University
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.
Amgen
Rare dipeptide and urea derivatives from roots of Moringa oleifera as potential anti-inflammatory and antinociceptive agents.
Central Drug Research Institute
Design and synthesis of indole-based peptoids as potent noncompetitive antagonists of transient receptor potential vanilloid 1.
University of Barcelona
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.
Amgen
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
Amgen
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
Glaxosmithkline
Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design.
Biocon-Bristol Myers Squibb Research and Development Centre
Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin.
Seoul National University
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Neurogen
The search for novel TRPV1-antagonists: from carboxamides to benzimidazoles and indazolones.
Merck Sharp & Dohme
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
Novartis Institutes For Biomedical Research
Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents.
Seoul National University
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
Seoul National University
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Seoul National University
-Methylamide-structured SB366791 derivatives with high TRPV1 antagonistic activity: toward PET radiotracers to visualize TRPV1.
Riken Center For Biosystems Dynamics Research
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.
Johnson & Johnson Pharmaceutical Research and Development
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands.
Seoul National University
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 activity.
Seoul National University
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.
Purdue Pharma
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.
Seoul National University
Paracetamol analogues conjugated by FAAH induce TRPV1-mediated antinociception without causing acute liver toxicity.
Lund University
Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.
Seoul National University
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
University of Nebraska Medical Center
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.
University of Concepcion
Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.
Sandoz Institute For Medical Research
Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
Seoul National University
Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists.
Seoul National University
2-Methylacrylamide as a bioisoster of thiourea group for 1,3-dibenzylthioureido TRPV1 receptor antagonists.
Sookmyung Women'S University
Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1).
National Cancer Institute-Bethesda
Vanilloid receptor ligands, pharmaceutical compositions containing them, process for making them, and use thereof for treating pain and other conditions
Gruenenthal
Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin.
Merck Sharp and Dohme Research Laboratories
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Amgen
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Amgen
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
Amgen
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.
Abbott Laboratories
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Seoul National University