0000000000053794

AUTHOR

A. Alavi

showing 3 related works from this author

Synthesis and evaluation of (S)-2-(2-[18F]fluoroethoxy)-4-([3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl-carbamoyl]-methyl)-benzoic acid ([18F]repaglin…

2004

18F-labeled non-sulfonylurea hypoglycemic agent (S)-2-(2-[(18)F]fluoroethoxy)-4-((3-methyl-1-(2-piperidin-1-yl-phenyl)-butylcarbamoyl)-methyl)-benzoic acid ([(18)F]repaglinide), a derivative of the sulfonylurea-receptor (SUR) ligand repaglinide, was synthesized as a potential tracer for the non-invasive investigation of the sulfonylurea 1 receptor status of pancreatic beta-cells by positron emission tomography (PET) in the context of type 1 and type 2 diabetes. [(18)F]Repaglinide could be obtained in an overall radiochemical yield (RCY) of 20% after 135 min with a radiochemical purity higher than 98% applying the secondary labeling precursor 2-[(18)F]fluoroethyltosylate. Specific activity w…

Fluorine RadioisotopesCancer ResearchBiodistributionMetabolic Clearance RateReceptors DrugContext (language use)Sulfonylurea ReceptorsRats Sprague-DawleyIslets of Langerhanschemistry.chemical_compoundPiperidinesmedicineRadioligandAnimalsTissue DistributionRadiology Nuclear Medicine and imagingPotassium Channels Inwardly RectifyingBenzoic acidChemistryBiological activityLigand (biochemistry)RepaglinideRatsDissociation constantBiochemistryOrgan SpecificityRats Inbred LewIsotope LabelingPositron-Emission TomographyFeasibility StudiesMolecular MedicineATP-Binding Cassette TransportersCarbamatesMultidrug Resistance-Associated ProteinsRadiopharmaceuticalsNuclear chemistrymedicine.drugNuclear Medicine and Biology
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Synthesis and first evaluation of new 18F-labelled sulfonylureas for the determination of the beta-cell status in vivo

2001

The syntheses and first in vitro evaluations for two fluoride bearing sulfonylurea derivatives are reported. Firstly, the tolbutamide derivative 1-[4-(2-[18F]fluoroethoxy)benzenesulfonyl]-3-butyl urea (2-[18F]fluoroethyl-tolbutamide) could be labeled efficiently with [18F]fluoride. Subsequently, the glibenclamid derivative N-(2-(4-(N-((cyclohexylamino)carbonyl)sulfonylamino)phenyl)ethyl) 2-(5-chloro-2-[18F]fluorethoxy)phenyl) formamide (2-[18F]fluoroethyl-glibenclamide) was labeled with [18F]fluoride in high yields. Its ability to induce insuline secretion from rat beta-cells in relation to the original glibenclamide was determined.

FormamideStereochemistrymedicine.drug_classOrganic ChemistryBiochemistrySulfonylureaIn vitroAnalytical ChemistryGlibenclamidechemistry.chemical_compoundTolbutamidechemistryIn vivoDrug DiscoveryUreamedicineRadiology Nuclear Medicine and imagingFluorideSpectroscopymedicine.drugJournal of Labelled Compounds and Radiopharmaceuticals
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Development and validation of the International Hidradenitis Suppurativa Severity Score System (IHS4), a novel dynamic scoring system to assess HS se…

2017

Background A validated tool for the dynamic severity assessment of hidradenitis suppurativa (HS) is lacking. The aim of this study was to develop and validate such a novel scoring system. Methods A Delphi voting procedure was conducted among the members of the European Hidradenitis Suppurativa Foundation (EHSF) to achieve consensus towards an initial HS Severity Score System (HS4). Strengths and weaknesses of HS4 were examined by a multicenter prospective study. Multivariate logistic regression, discriminant analysis and receiver operating characteristic curves and examination for correlation (Spearman's rho) and agreement (Cohen's kappa) with existing scores were engaged to recognize the v…

AdultMaleMultivariate statisticsmedicine.medical_specialtyConsensusDermatologyLogistic regressionSeverity of Illness Index030207 dermatology & venereal diseases03 medical and health sciences0302 clinical medicineInternal medicinemedicineHumansHidradenitis suppurativaProspective Studies610 Medicine & healthProspective cohort studyReceiver operating characteristicbusiness.industryOdds ratioDermatology Life Quality Indexmedicine.diseaseHidradenitis SuppurativaSurgery030220 oncology & carcinogenesisQuality of LifeFemaleSettore MED/35 - MALATTIE CUTANEE E VENEREEbusinessKappa
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