228 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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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
Partial Activation and Inhibition of TRPV1 Channels by Evodiamine and Rutaecarpine, Two Major Components of the Fruits of Evodia rutaecarpa.
TBA
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
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
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
a-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists.
Seoul National University
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
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
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
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
Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists.
Seoul National University
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
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
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
3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists.
Seoul National University
Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators.
Sapienza University of Rome
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
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
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
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Seoul National University
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
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
(-)-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
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
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
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
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
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
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
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
Amgen
Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain.
The First Affiliated Hospital of Zhengzhou University
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
Glaxosmithkline
-Guided Rational Drug Design and Synthesis of Novel 4-(Thiophen-2-yl)butanamides as Potent and Selective TRPV1 Agonists.
Magna Gracia University
Discovery of N-(1-(2-hydroxyethyl)quinolin-2-one)-N'-(1-phenyl-1H-pyrazol-5-yl)methyl) urea as Mode-Selective TRPV1 antagonist.
Seoul National University
Design, synthesis, and analgesia evaluation of novel Transient Receptor Potential Vanilloid 1 (TRPV1) agonists modified from Cannabidiol (CBD).
Shanghai University of Traditional Chinese Medicine
First-in-Class Dual Hybrid Carbonic Anhydrase Inhibitors and Transient Receptor Potential Vanilloid 1 Agonists Revert Oxaliplatin-Induced Neuropathy.
University of Florence
Transient Receptor Potential Melastatin 8 Channel (TRPM8) Modulation: Cool Entryway for Treating Pain and Cancer.
Instituto De Qu£Mica M£Dica
Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design.
Biocon-Bristol Myers Squibb Research and Development Centre
Synthesis and biological evaluation of N-(benzene sulfonyl)acetamide derivatives as anti-inflammatory and analgesic agents with COX-2/5-LOX/TRPV1 multifunctional inhibitory activity.
Anhui University of Chinese Medicine
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
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
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
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
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
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
-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
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Amgen
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
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
7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.
Johnson & Johnson Pharmaceutical Research and Development
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.
Purdue Pharma
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
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
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-α-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
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
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
University of Nebraska Medical Center
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
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
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
2-Methylacrylamide as a bioisoster of thiourea group for 1,3-dibenzylthioureido TRPV1 receptor antagonists.
Sookmyung Women'S 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
Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1).
National Cancer Institute-Bethesda
JAK kinase inhibitor compounds for treatment of respiratory disease
Theravance Biopharma R&D Ip
Phosphorus-substituted quinoxaline-type piperidine compounds and uses thereof
Purdue Pharma
Amino compounds for treatment of complement mediated disorders
Achillion Pharmaceuticals
Substituted 4,5,6,7-tetrahydropyrazolo[1,5-A]pyrazine derivatives as casein kinase 1 D/E inhibitors
Bristol-Myers Squibb
The evaluation of inhibitive effectiveness of the tumour necrosis factor-a converting enzyme selective inhibitors by HPLC.
Huazhong University of Science and Technology
Polar Hinges as Functionalized Conformational Constraints in (Bi)cyclic Peptides.
University of Glasgow
FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas.
The Scripps Research Institute
Therapeutic applications in the cardiovascular field of quinazolinedione derivatives
Sanofi
Characterization of isoprenaline- and salmeterol-stimulated interactions between beta2-adrenoceptors and beta-arrestin 2 using beta-galactosidase complementation in C2C12 cells.
Institute of Cell Signaling
In vitro and in vivo pharmacological characterization of BM-613 [N-n-pentyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist.
University of Li&Eagrove;Ge
Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons.
State University of New York
A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization.
Schering-Plough Research Institute
A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain.
Eli Lilly
Pharmacological and autoradiographic discrimination of sigma and phencyclidine receptor binding sites in brain with (+)-[3H]SKF 10,047, (+)-[3H]-3-[3-hydroxyphenyl]-N-(1-propyl)piperidine and [3H]-1-[1-(2-thienyl)cyclohexyl]piperidine.
The Johns Hopkins University
Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
UniversitÄT Heidelberg
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
Purdue University
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.
St. Jude Research Hospital
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
Merck Research Laboratories
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.
Cyclacel
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.
Cyclacel
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes.
Uppsala University