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A new chemical tool for exploring the physiological function of the PDE2 isozymeEvaluation of a Mathematical Model of Rat Body Weight Regulation in Application to Caloric Restriction and Drug Treatment StudiesQuantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) receptor antagonist.Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.Investigation of the CNS penetration of a potent 5-HT2a receptor antagonist (MDL 100,907) and an active metabolite (MDL 105,725) using in vivo microdialysis sampling in the rat.Structure-based drug metabolism predictions for drug design.Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.In Vitro-In Vivo Extrapolation of Intestinal Availability for Carboxylesterase Substrates Using Portal Vein-Cannulated Monkey.Rapid Method To Determine Intracellular Drug Concentrations in Cellular Uptake Assays: Application to Metformin in Organic Cation Transporter 1-Transfected Human Embryonic Kidney 293 Cells.Toward a unified model of passive drug permeation II: the physiochemical determinants of unbound tissue distribution with applications to the design of hepatoselective glucokinase activators.Passive drug permeation through membranes and cellular distribution.Strategic use of plasma and microsome binding to exploit in vitro clearance in early drug discovery.Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.Insights From an Integrated Physiologically Based Pharmacokinetic Model for Brain Penetration.Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles.Impact of Mrp2 on the biliary excretion and intestinal absorption of furosemide, probenecid, and methotrexate using Eisai hyperbilirubinemic rats.Towards a unified model of passive drug permeation I: origins of the unstirred water layer with applications to ionic permeation.Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice.Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor.Intravenous microdialysis sampling in awake, freely-moving rats.Comparison of in vitro BBMEC permeability and in vivo CNS uptake by microdialysis sampling.Extended Clearance Classification System (ECCS) informed approach for evaluating investigational drugs as substrates of drug transporters.Species independence in brain tissue binding using brain homogenatesMechanistic insights from comparing intrinsic clearance values between human liver microsomes and hepatocytes to guide drug designIn vivo microdialysis sampling coupled to liquid chromatography for the study of acetaminophen metabolismMicrodialysis-perfusion sampling for the investigation of phenol metabolismIn vivo microdialysis sampling for pharmacokinetic investigationsEnzymatic formation and electrochemical characterization of multiply substituted glutathione conjugates of hydroquinoneIn vivo microdialysis sampling in the bile, blood, and liver of rats to study the disposition of phenolQuantification of a dual angiotensin I-converting enzyme-neutral endopeptidase inhibitor and the active thiol metabolite in dog plasma by high-performance liquid chromatography with ultraviolet absorbance detectionPlasma pharmacokinetics of lactone and carboxylate forms of 20(S)-camptothecin in anesthetized ratsIn silico modeling of nonspecific binding to human liver microsomesDiscovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized ratsA nonprostanoid EP4 receptor selective prostaglandin E2 agonist restores bone mass and strength in aged, ovariectomized ratsExcretion, metabolism, and pharmacokinetics of CP-945,598, a selective cannabinoid receptor antagonist, in rats, mice, and dogsProjecting ADME Behavior and Drug-Drug Interactions in Early Discovery and Development: Application of the Extended Clearance Classification System
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description
hulumtues
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onderzoeker
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researcher
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հետազոտող
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name
Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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type
label
Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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prefLabel
Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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Dennis O. Scott
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P106
P1153
36017567900
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P31
P496
0000-0003-1385-6812