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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

Propentofylline attenuates tau hyperphosphorylation in Alzheimer's Swedish mutant model Tg2576
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Use of optically active cyclic diethyl sulfamidate 2-phosphonates as chiral synthons for the synthesis of β-substituted α-amino phosphonates
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Transport of the investigational anti-cancer drug 5,6-dimethylxanthenone-4-acetic acid and its acyl glucuronide by human intestinal Caco-2 cells
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Preparation and evaluation of glibenclamide-polyglycolized glycerides solid dispersions with silicon dioxide by spray drying technique
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Pharmacokinetic and pharmacodynamic modeling of recombinant human erythropoietin after multiple subcutaneous doses in healthy subjects
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Pluronic-g-poly(acrylic acid) copolymers as novel excipients for site specific, sustained release tablets
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Differential expression of P2X receptors on neurons from different parasympathetic ganglia
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Iron protects astrocytes from 6-hydroxydopamine toxicity
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Effect of acute and chronic psychostimulant drugs on redox status, AP-1 activation and pro-enkephalin mRNA in the human astrocyte-like U373 MG cells
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Reversal of caffeine-induced anxiety by neurosteroid 3-alpha-hydroxy-5-alpha-pregnane-20-one in rats
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Role of α7-nicotinic acetylcholine receptors in tetanic stimulation-induced γ oscillations in rat hippocampal slices
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Endocannabinoid release from midbrain dopamine neurons: a potential substrate for cannabinoid receptor antagonist treatment of addiction
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Phasic cardiovascular responses to mevinphos are mediated through differential activation of cGMP/PKG cascade and peroxynitrite via nitric oxide generated in the rat rostral ventrolateral medulla by NOS I and II isoforms
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A study of the enantiopreference of lipase PS (Pseudomonas cepacia) towards diastereomeric dihydro-5-alkyl-4-hydroxymethyl-2(3H)-furanones
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Cisplatin increases brain 2-arachidonoylglycerol (2-AG) and concomitantly reduces intestinal 2-AG and anandamide levels in the least shrew
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Neuronal Kir3.1/Kir3.2a channels coupled to serotonin 1A and muscarinic m2 receptors are differentially modulated by the 'short' RGS3 isoform
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Metabotropic glutamate receptor (mGluR5) antagonist MPEP attenuated cue- and schedule-induced reinstatement of nicotine self-administration behavior in rats
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Group II and III mGluRs-mediated presynaptic inhibition of EPSCs recorded from hippocampal interneurons of CA1 stratum lacunosum moleculare
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Group II mGluR-induced long term depression in the dentate gyrus in vivo is NMDA receptor-independent and does not require protein synthesis
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Antinociceptive effects of the antidepressants amitriptyline, duloxetine, mirtazapine and citalopram in animal models of acute, persistent and neuropathic pain
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The substituted aspartate analogue l-β-threo-benzyl-aspartate preferentially inhibits the neuronal excitatory amino acid transporter EAAT3
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Ncm-d-aspartate: A novel caged d-aspartate suitable for activation of glutamate transporters and N-methyl-d-aspartate (NMDA) receptors in brain tissue
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Effects of cinnarizine, a calcium antagonist that produces human parkinsonism, in parkin knock out mice
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Design of antagonists for NMDA and AMPA receptors
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Peripherally acting NMDA receptor/glycineB site receptor antagonists inhibit morphine tolerance
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Synthesis and anti-viral activity of a series of d- and l-2′-deoxy-2′-fluororibonucleosides in the subgenomic HCV replicon system
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Synthesis and characterization of EADAM: a selective radioligand for mapping the brain serotonin transporters by positron emission tomography
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Backbone metal-cyclization: a novel approach for simultaneous peptide cyclization and radiolabeling. Application to the combinatorial synthesis of rhenium-cyclic somatostatin analogs
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Modeling and analysis of PET studies with norepinephrine transporter ligands: the search for a reference region
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Picolylamine-methylphosphonic acid esters as tridentate ligands for the labeling of alcohols with the fac-[M(CO)3]+ core (M=99mTc, Re): synthesis and biodistribution of model compounds and of a 99mTc-labeled cobinamide
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MBP-annexin V radiolabeled directly with iodine-124 can be used to image apoptosis in vivo using PET
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Breast imaging: a surgeon's prospective
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New-generation radiotracers for nAChR and NET
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Structure-activity relationships for inhibition of human cholinesterases by alkyl amide phenothiazine derivatives
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Natural and synthetic cage compounds incorporating the 2,9,10-trioxatricyclo[4.3.1.03,8]decane type moiety
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Non-stochastic and stochastic linear indices of the 'molecular pseudograph's atom adjacency matrix': application to 'in silico' studies for the rational discovery of new antimalarial compounds
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Synthesis and biological evaluation of nucleobase-modified analogs of the anticancer compounds 3′-C-ethynyluridine (EUrd) and 3′-C-ethynylcytidine (ECyd)
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Modified mannose disaccharides as substrates and inhibitors of a polyprenol monophosphomannose-dependent α-(1→6)-mannosyltransferase involved in mycobacterial lipoarabinomannan biosynthesis
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Non-steroidal anti-inflammatory drugs have anti-amyloidogenic effects for Alzheimer's β-amyloid fibrils in vitro
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Structure-based discovery of human l-xylulose reductase inhibitors from database screening and molecular docking
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Design, synthesis, and evaluation of potent and selective benzoyleneurea-based inhibitors of protein geranylgeranyltransferase-I
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Chemo-enzymatic synthesis and cell-growth inhibition activity of resveratrol analogues
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Circular dichroism and absorption spectroscopic data reveal binding of the natural cis-carotenoid bixin to human α1-acid glycoprotein
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Formation of stacking complexes between caffeine (1,2,3-trimethylxanthine) and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine may attenuate biological effects of this neurotoxin
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Dinuclear macrocyclic polyamine zinc(II) complexes linked with flexible spacers: Synthesis, characterization, and DNA cleavage
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Structure and mechanism of tryptophylquinone enzymes
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Synthesis of gold nanoparticles bearing the Thomsen-Friedenreich disaccharide: a new multivalent presentation of an important tumor antigen
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Novel multivalent mannose compounds and their inhibition of the adhesion of type 1 fimbriated uropathogenic E. coli
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5-Thio-d-glycopyranosylamines and their amidinium salts as potential transition-state mimics of glycosyl hydrolases: synthesis, enzyme inhibitory activities, X-ray crystallography, and molecular modeling
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Synthesis and conformational analysis of novel water soluble macrocycles incorporating carbohydrates, including a β-cyclodextrin mimic
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Mapping the Dose-Effect Relationship of Orbofiban from Sparse Data with an Artificial Neural Network
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Dendrisomes: Vesicular Structures Derived from a Cationic Lipidic Dendron
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Complexation of celecoxib with β‐cyclodextrin: Characterization of the interaction in solution and in solid state
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A factor analysis for complex systems containing nimesulide
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Carrier mediated transport of chlorpheniramine and chlorcyclizine across bovine olfactory mucosa: Implications on nose‐to‐brain transport
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Reductase‐mediated metabolism of motexafin gadolinium (Xcytrin®) in rat and human liver subcellular fractions and purified enzyme preparations
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Effects of electrophoresis and electroosmosis during alternating current iontophoresis across human epidermal membrane
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Influence of the intermediate digestion phases of common formulation lipids on the absorption of a poorly water‐soluble drug
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Bioinspired applications of functional dendrimers
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Accidents médicamenteux
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Les médicaments radiopharmaceutiques
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Place actuelle des endoprothèses coronaires dans le traitement de la cardiopathie ischémique
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Place de la chimiothérapie de première ligne dans le cancer de l'ovaire
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Peroxide-Mediated Desulfurization of Phosphorothioate Oligonucleotides and Its Prevention
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Characterization of Physico-Mechanical Properties of Indomethacin and Polymers to Assess their Suitability for Hot-Melt Extrusion Processs as a Means to Manufacture Solid Dispersion/Solution*
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Evaluation of pig esophageal mucosa as a permeability barrier model for buccal tissue
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Significant differences in the disposition of cyclic prodrugs of opioid peptides in rats and guinea pigs following IV administration
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Dose dependency in the oral bioavailability of an organic cation model, tributylmethyl ammonium (TBuMA), in rats: Association with the saturation of efflux by the P-gp system on the apical membrane of the intestinal epithelium
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Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists
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Geldanamycin derivative inhibition of HGF/SF-mediated Met tyrosine kinase receptor-dependent urokinase-plasminogen activation
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Preventive effects of soyasapogenol B derivatives on liver injury in a concanavalin A-induced hepatitis model
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Exploration of orally available calpain inhibitors: Peptidyl α-ketoamides containing an amphiphile at P3 site
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Dirhodium tetraacetate as an auxiliary chromophore in a circular dichroic study on vic-amino alcohols
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Quinoid BINOL-type compounds as a novel class of chiral ligands
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An efficient approach to enantiomeric isoxazolidinyl analogues of tiazofurin based on nitrone cycloadditions
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Pharmacokinetic Effects of 4C9, An Anti-FcRn Antibody, in Rats: Implications for the Use of FcRn Inhibitors for the Treatment of Humoral Autoimmune and Alloimmune Conditions
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Down-regulation of the glial glutamate transporter GLT-1 in rat hippocampus and striatum and its modulation by a group III metabotropic glutamate receptor antagonist following transient global forebrain ischemia
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Repeated exposure to Δ9-tetrahydrocannabinol alters heroin-induced locomotor sensitisation and Fos-immunoreactivity
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Glycinergic inhibition in thalamus revealed by synaptic receptor blockade
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Excessive crying and gastro-oesophageal reflux disease in infants: misalignment of biology and culture
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Calcium-mediated aponecrosis plays a central role in the pathogenesis of estrogenic chemical-induced neurotoxicity
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Metabolic depression in hibernation and major depression: An explanatory theory and an animal model of depression
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A possible explanation for the racial difference in distribution of large-arterial cerebrovascular disease: Ancestral European settlers evolved genetic resistance to atherosclerosis, but confined to the intracranial arteries
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Intrinsic toxicity of glucose, due to non-enzymatic glycation, is controlled in-vivo by deglycation systems including: FN3K-mediated deglycation of fructosamines and transglycation of aldosamines
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The impact of the transmission dynamics of the HIV/AIDS epidemic on sexual behaviour: A new hypothesis to explain recent increases in risk taking-behaviour among men who have sex with men
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Multiple sclerosis and hepatitis B vaccination: Could minute contamination of the vaccine by partial Hepatitis B virus polymerase play a role through molecular mimicry?
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Water Adsorption Kinetics and Contact Angles of Pharmaceutical Powders
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Partially Crystalline Systems in Lyophilization: II. Withstanding Collapse at High Primary Drying Temperatures and Impact on Protein Activity Recovery
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Synthesis of disparlure analogues, using resolution on microcrystalline cellulose triacetate-I
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Single Crystal and Powder Diffraction Characterization of Three Polymorphic Forms of Acitretin
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The Effect of Water to Ethanol Feed Ratio on Physical Properties and Aerosolization Behavior of Spray Dried Cromolyn Sodium Particles
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Microdialysis evaluation of the brain distribution of stavudine following intranasal and intravenous administration to rats
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Surface roughness contribution to the adhesion force distribution of salmeterol xinafoate on lactose carriers by atomic force microscopy
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Effect of the covalent modification of horseradish peroxidase with poly(ethylene glycol) on the activity and stability upon encapsulation in polyester microspheres
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Intracellular delivery of doxorubicin with RGD-modified sterically stabilized liposomes for an improved antitumor efficacy: In vitro and in vivo
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Lipid Binding Region (2303-2332) is Involved in Aggregation of Recombinant Human FVIII (rFVIII)*
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Tissue Distribution of Basic Drugs: Accounting for Enantiomeric, Compound and Regional Differences Amongst β-Blocking Drugs in Rat
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Pharmacokinetic Study of Methotrexate Following Intra-Articular Injection of Methotrexate Loaded Poly(L-Lactic Acid) Microspheres in Rabbits
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Versatile Peptide Dendrimers for Nucleic Acid Delivery
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Pharmacokinetics and Metabolism of Metoprolol and Propranolol in the Female DA and Female Wistar Rat: The Female DA Rat Is Not Always an Animal Model for Poor Metabolizers of CYP2D6
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