PMID

Data

Article Title

Organization

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

Discovery of TRPV1 antagonist ABT-116.

Abbott Laboratories

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

Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.

Amgen

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

Synthesis of benzamide derivatives as TRPV1 antagonists.

Pfizer

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

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

Radiofluorinated N-Octanoyl Dopamine ([

Mannheim University Of Applied Sciences

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

TRPV1 Modulators for the Treatment of Pain and Inflammation.

Usona Institute

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

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

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

High affinity antagonists of the vanilloid receptor.

National Cancer Institute-Bethesda

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

Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.

Seoul National University