Search results for "Oates"

showing 5 items of 145 documents

Safety and tolerability of β3-adrenoceptor agonists in the treatment of overactive bladder syndrome - insight from transcriptosome and experimental s…

2016

We have reviewed the safety and tolerability of β3-adrenoceptor agonists, specifically mirabegron and solabegron, a newly emerging drug class for the treatment of the overactive bladder syndrome. We discuss them mechanistically in the context of expression and other preclinical data.Based on a systematic PubMed search, incidence of overall adverse events, hypertension, dry mouth, and constipation are comparable between mirabegron or solabegron and placebo. Hypertension is the most frequently observed adverse event, but has a similar incidence with mirabegron and placebo. Nevertheless, severe uncontrolled hypertension has become a contraindication for use of mirabegron based on observation o…

medicine.medical_specialtySide effect030232 urology & nephrologyUrologyContext (language use)Adrenergic beta-3 Receptor AgonistsBenzoates03 medical and health sciences0302 clinical medicineSolabegronmedicineAnimalsHumansPharmacology (medical)Adverse effectAniline Compoundsbusiness.industryUrinary Bladder OveractiveGene Expression ProfilingBiphenyl CompoundsGeneral MedicineBiphenyl compoundThiazolesTolerability030220 oncology & carcinogenesisAnesthesiaReceptors Adrenergic beta-3AcetanilidesTolterodinebusinessMirabegronmedicine.drugExpert opinion on drug safety
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Direct Visualization of Molecule Deprotonation on an Insulating Surface

2012

Elucidating molecular-scale details of basic reaction steps on surfaces is decisive for a fundamental understanding of molecular reactivity within many fields, including catalysis and on-surface synthesis. Here, the deprotonation of 2,5-dihydroxybenzoic acid (DHBA) deposited onto calcite (101;4) held at room temperature is followed in situ by noncontact atomic force microscopy. After deposition, the molecules form two coexisting phases, a transient striped phase and a stable dense phase. A detailed analysis of high-resolution noncontact atomic force microscopy images indicates the transient striped phase being a bulk-like phase, which requires hydrogen bonds between the carboxylic acid moie…

noncontact atomic force microscopyCarboxylic acidCatecholsGeneral Physics and AstronomyMicroscopy Atomic ForceKelvin probe force microscopy530Calcium Carbonatechemistry.chemical_compoundDeprotonationPhase (matter)Materials TestingHydroxybenzoatesMoleculeGeneral Materials ScienceReactivity (chemistry)CarboxylateParticle Sizechemistry.chemical_classificationKelvin probe force microscopeHydrogen bondinsulating surfaceGeneral EngineeringElectric ConductivityMolecular ImagingNanostructuresCrystallographychemistrydeprotonationProtons
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Compatibilization of Polylactide/Poly(ethylene 2,5-furanoate) (PLA/PEF) Blends for Sustainable and Bioderived Packaging.

2022

Despite the advantages of polylactide (PLA), its inadequate UV-shielding and gas-barrier properties undermine its wide application as a flexible packaging film for perishable items. These issues are addressed in this work by investigating the properties of melt-mixed, fully bioderived blends of polylactide (PLA) and poly(ethylene furanoate) (PEF), as a function of the PEF weight fraction (1–30 wt %) and the amount of the commercial compatibilizer/chain extender Joncryl ADR 4468 (J, 0.25–1 phr). J mitigates the immiscibility of the two polymer phases by decreasing and homogenizing the PEF domain size; for the blend containing 10 wt % of PEF, the PEF domain size drops from 0.67 &p…

poly(ethylene furanoate)compatibilizationPolymersPolyestersOrganic ChemistryPharmaceutical ScienceEthylenesfuranoatesAnalytical ChemistryOxygenSettore ING-IND/22 - Scienza E Tecnologia Dei MaterialiBlendsgas-permeabilityChemistry (miscellaneous)PolyethylenepolylactideDrug DiscoveryblendsMolecular Medicinepolylactide; furanoates; poly(ethylene furanoate); blends; compatibilization; gas-permeability; UV-shieldingUV-shieldingPhysical and Theoretical ChemistryMolecules (Basel, Switzerland)
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Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action

2015

Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsins B and L, and were found to be potent and selective inhibitors of rhodesain. Among them (S,E)-ethyl 5-((S)-2-{[(benzyloxy)carbonyl]amino}-3-phenylpropanamido)-7-methyl-4-oxooct-2-enoate (6) was the most potent, with an IC50 value of 16.4 nm and kinact/Ki=1.6×106 m−1 s−1 against rhodesain. These dipeptidyl enoates display a reversible mode of inhibition at very low concentrations and an irreversible mode at higher concentrations. Inhibition…

trypanosomiasisStereochemistrysleeping sicknessCathepsin LDrug Evaluation PreclinicalChemistry Techniques SyntheticInhibition kineticsCysteine Proteinase InhibitorsBiochemistryCathepsin BInhibitory Concentration 50Structure-Activity RelationshipinhibitorsDrug DiscoveryHumansMoietyMolecular Targeted TherapyGeneral Pharmacology Toxicology and PharmaceuticsIC50Volume concentrationrhodesainPharmacologyChemistryOrganic ChemistryDual modeDipeptidesTrypanocidal AgentsCombinatorial chemistryMolecular Docking SimulationCysteine EndopeptidasesKineticsdipeptidyl enoatesTrypanosomiasis AfricanDocking (molecular)Molecular MedicineCysteine thiolateChemMedChem
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Biopolymer Recovery from Aerobic Granular Sludge and Conventional Flocculent Sludge in Treating Industrial Wastewater: Preliminary Analysis of Differ…

2022

The recovery of biopolymers from sewage sludge could be a crucial step in implementing circular economy principles in wastewater treatment plants (WWTP). In this frame, the present study was aimed at evaluating the simultaneous production of polyhydroxyalkanoates (PHA) and extracellular polymeric substances (EPS) obtainable from the treatment of agro-industrial wastewater. Two biological enrichment systems, aerobic granular sludge (AGS) and a conventional activated sludge operating as a sequencing batch reactor (SBR), were monitored for 204 and 186 days, respectively. The maximum biopolymers accumulation capacity was close to 0.60 mgPHA-EPS gVSS−1 in the AGS when operating at 3 kgCODm…

wastewater treatmentsewage sludgeSettore ICAR/03 - Ingegneria Sanitaria-Ambientalebiopolymercircular economyaerobic granular sludge; biopolymers; circular economy; extracellular polymeric substances; polyhydroxyalkanoates; sewage sludge; wastewater treatmentGeography Planning and Developmentpolyhydroxyalkanoateaerobic granular sludgeAquatic Scienceextracellular polymeric substanceBiochemistryWater Science and TechnologyWater
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