63 articles for thisTarget
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Article Title
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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
Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators.
University of Salerno
Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.
Pfizer
Structure-activity relationships of the prototypical TRPM8 agonist icilin.
National Research Council
Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives.
University of Shizuoka
Effect of acyclic monoterpene alcohols and their derivatives on TRP channels.
Sapienza University of Rome
Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist.
Raqualia Pharma
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
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Amgen
Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree.
University of Shizuoka
Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists.
Pfizer
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
3-Ylidenephthalides as a new class of transient receptor potential channel TRPA1 and TRPM8 modulators.
Sapienza University of Rome
Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.
Sapienza University of Rome
Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.
Amgen
Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists.
Janssen Pharmaceutica
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 vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia.
Janssen Pharmaceutica
Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa).
Universita` Del Piemonte Orientale
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
TRPM8 voltage sensor mutants reveal a mechanism for integrating thermal and chemical stimuli.
Ku Leuven
(-)-Menthylamine derivatives as potent and selective antagonists of transient receptor potential melastatin type-8 (TRPM8) channels.
Sapienza University of Rome
Taste-guided identification of high potency TRPA1 agonists from Perilla frutescens.
Università
Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich
University of Naples Federico Ii
-Guided Rational Drug Design and Synthesis of Novel 4-(Thiophen-2-yl)butanamides as Potent and Selective TRPV1 Agonists.
Magna Gracia University
Discovery of Novel TRPM8 Blockers Suitable for the Treatment of Somatic and Ocular Painful Conditions: A Journey through p
Dompe Farmaceutici
Transient Receptor Potential Melastatin 8 Channel (TRPM8) Modulation: Cool Entryway for Treating Pain and Cancer.
Instituto De Qu£Mica M£Dica
Discovery of (S)-N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist.
Henan University
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
New TRPM8 blockers exert anticancer activity over castration-resistant prostate cancer models.
University of Salerno
Design, synthesis and biological evaluation of new thiazole scaffolds as potential TRPM8 antagonists.
Dipartimento Di Scienze Fisiche E Chimiche Universit£
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
Peking University
Structural and in Vitro Functional Characterization of a Menthyl TRPM8 Antagonist Indicates Species-Dependent Regulation.
Marshall University
Identification of N-acyl-N-indanyl-α-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects.
Kissei Pharmaceutical
Exploration of TRPM8 Binding Sites by β-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities.
University of Salerno
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
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
N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
University of Hull
Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity.
University of Salerno
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
Iodine-mediated cyclization of cannabigerol (CBG) expands the cannabinoid biological and chemical space.
University of Naples Federico II
Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).
TBA
Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors.
Peking University
Iodine-Promoted Aromatization of p-Menthane-Type Phytocannabinoids.
University of Eastern Piedmont
Discovery and development of a novel class of phenoxyacetyl amides as highly potent TRPM8 agonists for use as cooling agents.
Senomyx
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
6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof
Jiangsu Hengrui Medicine
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