[1]JournalofMedicinalChemistry,2007,vol.50,p.3515-3527
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[1]JournalofMedicinalChemistry,2007,vol.50,p.3515-3527
[1]JournalofMedicinalChemistry,2007,vol.50,p.3515-3527
[1]JournalofMedicinalChemistry,2007,vol.50,p.3515-3527
Title: 7-tert-Butyl-6-(4-chloro-phenyl)-2-thioxo-2,3-dihydro-1H-pyrido[2,3-d]pyrimidin-4-one, a classic polymodal inhibitor of transient receptor potential vanilloid type 1 with a reduced liability for hyperthermia, is analgesic and ameliorates visceral hypersensitivity.
Journal: The Journal of pharmacology and experimental therapeutics 20120801
Title: Aging reverses the role of the transient receptor potential vanilloid-1 channel in systemic inflammation from anti-inflammatory to proinflammatory.
Journal: Cell cycle (Georgetown, Tex.) 20120115
Title: TRPV1 antagonists: clinical setbacks and prospects for future development.
Journal: Progress in medicinal chemistry 20120101
Title: Application of automated serial blood sampling and dried blood spot technique with liquid chromatography-tandem mass spectrometry for pharmacokinetic studies in mice.
Journal: Journal of pharmaceutical and biomedical analysis 20111101
Title: Application of automated dried blood spot sampling and LC-MS/MS for pharmacokinetic studies of AMG 517 in rats.
Journal: Bioanalysis 20111001
Title: Improved pharmacokinetics of AMG 517 through co-crystallization part 2: analysis of 12 carboxylic acid co-crystals.
Journal: Journal of pharmaceutical sciences 20110701
Title: Improved pharmacokinetics of AMG 517 through co-crystallization. Part 1: comparison of two acids with corresponding amide co-crystals.
Journal: Journal of pharmaceutical sciences 20100901
Title: Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
Journal: Journal of medicinal chemistry 20100422
Title: Manufacture of pharmaceutical co-crystals using twin screw extrusion: a solvent-less and scalable process.
Journal: Journal of pharmaceutical sciences 20100401
Title: Analgesic potential of TRPV1 antagonists.
Journal: Biochemical pharmacology 20090801
Title: Characterization and optimization of AMG 517 supersaturatable self-emulsifying drug delivery system (S-SEDDS) for improved oral absorption.
Journal: Journal of pharmaceutical sciences 20090201
Title: Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.
Journal: Bioorganic & medicinal chemistry letters 20080915
Title: The co-crystal approach to improve the exposure of a water-insoluble compound: AMG 517 sorbic acid co-crystal characterization and pharmacokinetics.
Journal: Journal of pharmaceutical sciences 20080901
Title: Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.
Journal: Journal of medicinal chemistry 20080508
Title: Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans.
Journal: Pain 20080501
Title: On the thermoregulatory perils of TRPV1 antagonism.
Journal: Pain 20080501
Title: 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Journal: Bioorganic & medicinal chemistry letters 20080315
Title: Enhanced bioavailability of a poorly soluble VR1 antagonist using an amorphous solid dispersion approach: a case study.
Journal: Molecular pharmaceutics 20080101
Title: Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.
Journal: Bioorganic & medicinal chemistry letters 20071201
Title: Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
Journal: The Journal of pharmacology and experimental therapeutics 20071001
Title: Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Journal: Journal of medicinal chemistry 20070726
Title: Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Journal: Journal of medicinal chemistry 20070726
Title: Doherty EM, et al. Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J Med Chem. 2007 Jul 26;50(15):3515-27.
Title: Gavva NR, et al. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther. 2007 Oct;323(1):128-37.
