0000000000053794
AUTHOR
A. Alavi
Synthesis and evaluation of (S)-2-(2-[18F]fluoroethoxy)-4-([3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl-carbamoyl]-methyl)-benzoic acid ([18F]repaglinide): a promising radioligand for quantification of pancreatic β-cell mass with positron emission tomography (PET)
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…
Development and validation of the International Hidradenitis Suppurativa Severity Score System (IHS4), a novel dynamic scoring system to assess HS severity
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…
Synthesis and first evaluation of new 18F-labelled sulfonylureas for the determination of the beta-cell status in vivo
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.