6533b7defe1ef96bd127662f
RESEARCH PRODUCT
Synthesis and first evaluation of new 18F-labelled sulfonylureas for the determination of the beta-cell status in vivo
S. J. ShiueRalf SchirrmacherPeter J. FeilenStephan SchneiderA. AlaviFrank RöschGrace G. ShiueJürgen Beyersubject
FormamideStereochemistrymedicine.drug_classOrganic ChemistryBiochemistrySulfonylureaIn vitroAnalytical ChemistryGlibenclamidechemistry.chemical_compoundTolbutamidechemistryIn vivoDrug DiscoveryUreamedicineRadiology Nuclear Medicine and imagingFluorideSpectroscopymedicine.drugdescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2001-05-01 | Journal of Labelled Compounds and Radiopharmaceuticals |