0000000000774459

AUTHOR

Ignatz Wessler

showing 3 related works from this author

Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([18F…

2003

The 18 F-labeled b2-adrenergic receptor ligand (R,R)(S,S) 5-(2-(2-(4-(2-( 18 F)fluoroethoxy)phenyl)-1-methylethylamino)-1- hydroxyethyl)-benzene-1,3-diol, a derivative of the original highly selective racemic fenoterol, was synthesized in an overall radio- chemical yield of 20% after 65 min with a radiochemical purity higher than 98%. The specific activity was in the range of 50-60 GBq/mmol. In vitro testing of the non-radioactive fluorinated fenoterol derivative with isolated guinea pig trachea was conducted to obtain an IC50 value of 60 nM. Preliminary ex vivo organ distribution and in vivo experiments with positron emission tomography (PET) on guinea pigs were performed to study the biod…

Fluorine RadioisotopesBiodistributionSwineStereochemistryClinical BiochemistryDiolPharmaceutical ScienceIn Vitro TechniquesBiochemistryChemical synthesisGuinea pigchemistry.chemical_compoundIn vivoDrug DiscoverymedicineAnimalsTissue DistributionLungMolecular BiologyFenoterolFenoterolOrganic ChemistryLigand (biochemistry)Models ChemicalchemistryMolecular MedicineReceptors Adrenergic beta-2RadiopharmaceuticalsEx vivoTomography Emission-Computedmedicine.drugBioorganic & Medicinal Chemistry Letters
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Synthesis of [18F]-Fluoroethylfenoterol for imaging β2 receptor status in lung in vivo

2001

5-(-{2-[4-(2-[18F]Fluoroethoxy)-phenyl]-l-methyl-ethylamino}-l-hydroxy-ethyl)-benzene-1, 3-diol ([18F]fluoroethylfenoterol) was synthesised from 4-(2-{benzyl-[2-(3,5-bis-benzyloxy-phenyl)-2-hydroxy-ethyl]-amino}-propyl)-phenol using 2-[18F]fluoroethyltosylate (92% RCY) followed by reductive cleavage of the benzyl protecting groups. Preliminary in vitro tests showed [19F]fluoroethylfenoterol to be as potent in relaxation of lung tissue as fenoterol itself.

Receptor StatusLungChemistryorganic chemicalsOrganic ChemistryBiochemistryIn vitroAnalytical Chemistrymedicine.anatomical_structureIn vivoReductive cleavageDrug Discoverypolycyclic compoundsmedicineBiophysicsRelaxation (physics)heterocyclic compoundsRadiology Nuclear Medicine and imagingLung tissueSpectroscopyFenoterolmedicine.drugJournal of Labelled Compounds and Radiopharmaceuticals
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Administration of keratinocyte growth factor down-regulates the pulmonary capacity of acetylcholine production.

2007

Abstract Keratinocyte growth factor protects the lung against various injurious stimuli. The protective mechanisms, however, are not yet fully understood. The aim of this study is to determine the influence of keratinocyte growth factor on the pulmonary capacity to synthesize acetylcholine, a potent regulator of pulmonary functions which is potentially involved in lung damage. Rats were treated twice (days 1 and 2) intratracheally with keratinocyte growth factor and analyzed at day 4. The mRNA expression of choline acetyltransferase – the acetylcholine synthesizing enzyme – was analyzed by real-time RT-PCR in the lung and in isolated alveolar epithelial type II cells. Choline acetyltransfer…

Malemedicine.medical_specialtyFibroblast Growth Factor 7CellDown-RegulationBiologyBiochemistryCholine O-Acetyltransferasechemistry.chemical_compoundInternal medicinemedicineAnimalsRNA MessengerCation Transport ProteinsLungSurfactant homeostasisLungEpithelial CellsPulmonary SurfactantsCell BiologyCholine acetyltransferaseAcetylcholineRecombinant ProteinsRatsCholine transporterEndocrinologymedicine.anatomical_structurechemistryRats Inbred LewKeratinocyte growth factorKeratinocyteAcetylcholinemedicine.drugThe international journal of biochemistrycell biology
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