PMID

Data

Article Title

Organization

Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.

Glaxosmithkline

Synthesis and optimization of novela-phenylglycinamides as selective TRPM8 antagonists.

Kissei Pharmaceutical

Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1.

Shionogi

Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template.

Seoul National University

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.

Amgen

Arylboronic acids as dual-action FAAH and TRPV1 ligands.

Sapienza University of Rome

2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.

Seoul National University

TRPA1 channels as targets for resveratrol and related stilbenoids.

Sapienza University of Rome

Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.

Seoul National University

Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.

Renovis

Discovery of non-electrophilic capsaicinoid-type TRPA1 ligands.

University of Eastern Piedmont

Structure-Activity Relationship Study on Isothiocyanates: Comparison of TRPA1-Activating Ability between Allyl Isothiocyanate and Specific Flavor Components of Wasabi, Horseradish, and White Mustard.

University of Shizuoka

a-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists.

Seoul National University

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

Structure-activity relationships of the prototypical TRPM8 agonist icilin.

National Research Council

Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

Seoul National University

6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.

Shenyang Pharmaceutical University

Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.

Abbvie

Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist.

University of Siena

2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.

Seoul National University

2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.

Seoul National University

Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives.

University of Shizuoka

Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.

Roseman University of Health Sciences

Effect of acyclic monoterpene alcohols and their derivatives on TRP channels.

Sapienza University of Rome

Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists.

Genomics Institute of The Novartis Research Foundation

Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists.

Astrazeneca

Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.

Arena Pharmaceuticals

Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree.

University of Shizuoka

Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands.

Seoul National University

Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists.

Glenmark Pharmaceuticals

TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides.

Seoul National University

The carbonate analogues of 5'-halogenated resiniferatoxin as TRPV1 ligands.

Seoul National University

The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.

Glaxosmithkline

2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists: structure activity relationships of the 2-oxy pyridine C-region.

Seoul National University

Discovery of potent transient receptor potential vanilloid 1 antagonists: design and synthesis of phenoxyacetamide derivatives.

Toray Industries

Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring.

Sapienza University of Rome

Novel acylethanolamide derivatives that modulate body weight through enhancement of hypothalamic pro-opiomelanocortin (POMC) and/or decreased neuropeptide Y (NPY).

Hebrew University of Jerusalem

Tetrahydro-ß-carboline derivatives targeting fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channels.

Sapienza University of Rome

Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.

Merck Research Laboratories

Identification of potent, soluble, and orally active TRPV1 antagonists.

Msd

In vitro TRPV1 activity of piperine derived amides.

Universidad De Antioquia

2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region.

Seoul National University

Discovery of novel pyrrolopyridazine scaffolds as transient receptor potential vanilloid (TRPV1) antagonists.

Astrazeneca

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.

Astrazeneca

N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.

Seoul National University

Tetrahydro-naphthols as orally available TRPV1 inhibitors.

Bayer Yakuhin

Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.

Abbott Laboratories

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

Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): The side chain benzylic methylene.

University of Eastern Piedmont

New tetrazole-based selective anandamide uptake inhibitors.

Sapienza University of Rome

N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1).

Johnson & Johnson Pharmaceutical Research and Development

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.

Amgen

Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): the homovanillyl moiety.

University of Eastern Piedmont

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

Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor.

Johnson & Johnson Pharmaceutical Research and Development

Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators.

Sapienza University of Rome

Novel bioactive metabolites of dipyrone (metamizol).

Philipps-Universit£T

Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa).

Universita` Del Piemonte Orientale

Nobilamides A-H, long-acting transient receptor potential vanilloid-1 (TRPV1) antagonists from mollusk-associated bacteria.

University of Utah

Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence.

Bayer Yakuhin

Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.

Abbott Laboratories

Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.

Merck Sharpe and Dohme

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

Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.

Abbott Laboratories

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

(-)-Menthylamine derivatives as potent and selective antagonists of transient receptor potential melastatin type-8 (TRPM8) channels.

Sapienza University of Rome

Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands.

Sapienza University of Rome

 

Thiourea analogues of resiniferatoxin as ligands for the vanilloid receptor

TBA

Spiro-piperidine azetidinones as potent TRPV1 antagonists.

Schering-Plough Research Institute

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

Discovery of piperidine carboxamide TRPV1 antagonists.

Johnson & Johnson Pharmaceutical Research and Development

Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.

Neurogen

Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.

Amgen

Biologically active compounds from Aphyllophorales (polypore) fungi.

The University of Mississippi

Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.

Abbott Laboratories

Synthesis of benzamide derivatives as TRPV1 antagonists.

Pfizer

Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety.

Pfizer

Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.

Johnson & Johnson Pharmaceutical Research and Development

The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.

Glaxosmithkline

From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.

Neurogen

N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.

Glaxosmithkline

Discovery of (S)-N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist.

Henan University

Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.

University of Piemonte Orientale

The search for novel TRPV1-antagonists: from carboxamides to benzimidazoles and indazolones.

Merck Sharp & Dohme

The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent.

Turning Point Therapeutics

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

Discovery of Potent and Selective Transient Receptor Potential Vanilloid 1 (TRPV1) Agonists with Analgesic Effects

Fudan University

The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination.

University of Piemonte Orientale

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.

Indian Institute of Technology (B.H.U.)

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

4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists.

Purdue Pharma

Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.

Amgen

Phytocannabinoid Pharmacology: Medicinal Properties of

Scientus Pharma

Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.

Purdue Pharma

N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.

Johnson & Johnson Pharmaceutical Research and Development

7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.

Johnson & Johnson Pharmaceutical Research and Development

From High-Throughput Screening to Target Validation: Benzo[

Aptuit, An Evotec

2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists.

Seoul National University

Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift.

Seoul National University

Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.

University of Nebraska Medical Center

Discovery of a Remarkable Methyl Shift Effect in the Vanilloid Activity of Triterpene Amides.

National Research Council (Icb-Cnr)

Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists.

Seoul National University

Identification of N-acyl-N-indanyl-?-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects.

Kissei Pharmaceutical

Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide.

Henan University

Cannabitwinol, a Dimeric Phytocannabinoid from Hemp,

University of Naples Federico Ii

Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.

University of Siena

Discovery of indane propanamides as potent and selective TRPV1 antagonists.

Seoul National University

Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents.

National Research Council

Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.

Seoul National University

Capsaicin-like analogue induced selective apoptosis in A2058 melanoma cells: Design, synthesis and molecular modeling.

University of S£O Paulo

Onydecalins, Fungal Polyketides with Anti- Histoplasma and Anti-TRP Activity.

University of Utah

Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.

TBA

Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.

Seoul National University

Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists.

Henan University

Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.

Julius Maximilian University of W£Rzburg

Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1.

Henan University

Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse?

Hospital of The University of Pennsylvania

N-Acylvanillamides: development of an expeditious synthesis and discovery of new acyl templates for powerful activation of the vanilloid receptor.

Istituto Per La Chimica Di Molecole Di Interesse Biologico

Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists.

National Research Council (Cnr)

Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.

TBA

Novel benzodiazepines derivatives as analgesic modulating for Transient receptor potential vanilloid 1.

Chongqing Medical University

4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands.

Seoul National University

Iodine-mediated cyclization of cannabigerol (CBG) expands the cannabinoid biological and chemical space.

University of Naples Federico II

Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) Channel Softly: The Discovery of Passerini Adducts as a Topical Treatment for Inflammatory Skin Disorders.

University of Eastern Piedmont

Analyses of Synthetic N-Acyl Dopamine Derivatives Revealing Different Structural Requirements for Their Anti-inflammatory and Transient-Receptor-Potential-Channel-of-the-Vanilloid-Receptor-Subfamily-Subtype-1 (TRPV1)-Activating Properties.

Mannheim University of Applied Sciences

Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide.

China Pharmaceutical University

Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

Seoul National University

Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).

TBA

Iodine-Promoted Aromatization of p-Menthane-Type Phytocannabinoids.

University of Eastern Piedmont

Design, synthesis, and biological evaluation of novel biphenyl-4-carboxamide derivatives as orally available TRPV1 antagonists.

Astellas Pharma

Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists.

Seoul National University

Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain.

Shionogi

Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

Pharmaron-Beijing

t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

Seoul National University

Discovery of a Series of Indazole TRPA1 Antagonists.

Pfizer

Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1).

National Cancer Institute-Bethesda

1,3-substituted cyclobutyl derivatives and uses thereof

Novartis

hTRPV1 chemical agents

University of Pittsburgh

2-aryl-4-hydroxy-1,3-thiazole derivatives useful as TRPM8-inhibitors in treatment of neuralgia, pain, COPD and asthma

DompÉ

Substituted oxazole- and thiazole-based carboxamide and urea derivatives as vanilloid receptor ligands II

Medifron Dbt

Tetrahydro-pyrimidoazepines as modulators of TRPV1

Janssen Pharmaceutica

TRPV1 antagonists including dihydroxy substituent and uses thereof

Purdue Pharma

Tetrahydro-pyrimidoazepines as modulators of TRPV1

Janssen Pharmaceutica

TRPV1 antagonists including dihydroxy substituent and uses thereof

Purdue Pharma

TRPV1 antagonists including dihydroxy substituent and uses thereof

Purdue Pharma

TRPV1 antagonists including dihydroxy substituent and uses thereof

Purdue Pharma

Treatment of respiratory disorders using TRPA1 antagonists

Glenmark Pharmaceuticals

Compounds of modulating TRPV3 function

Hydra Biosciences

Heterocyclic compounds

Shionogi

Substituted phenylureas and phenylamides as vanilloid receptor ligands

Gruenenthal

TRPV1 antagonists

Abbvie

Aryl or N-heteroaryl substituted methanesulfonamide derivatives as vanilloid receptor ligands

Gruenenthal

Compounds having TRPV1 antagonistic activity and uses thereof

Shionogi

TRPV1 antagonists

Abbvie

TRPV1 antagonists

TBA

Vanilloid receptor ligands, pharmaceutical compositions containing them, process for making them, and use thereof for treating pain and other conditions

Gruenenthal

Amine substituted methanesulfonamide derivatives as vanilloid receptor ligands

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

Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.

Universita Del Piemonte Orientale

New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain.

Sapienza University of Rome

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

Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.

Gsk

Discovery of small molecule antagonists of TRPV1.

Gsk

[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.

Abbott Laboratories

Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.

Abbott Laboratories

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-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.

Abbott Laboratories

In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.

Abbott Laboratories