6533b7cffe1ef96bd1258fc6

RESEARCH PRODUCT

Total synthesis and evaluation of [18F]MHMZ.

Hartmut LüddensFrank RöschGitte M. KnudsenMarkus PielFabian DebusMikael PalnerMatthias M. Herth

subject

Fluorine RadioisotopesStereochemistryClinical BiochemistryPharmaceutical ScienceBiochemistryBinding CompetitiveRadioligand AssayPiperidinesIn vivoDrug DiscoveryAnimalsRadionuclide imagingReceptor Serotonin 5-HT2ARadionuclide ImagingMolecular BiologyChemistryOrganic ChemistrySynthonTotal synthesisBrainBiological activityRadioligand AssayRatsFluorobenzenesKineticsYield (chemistry)Isotope LabelingSerotonin 5-HT2 Receptor AntagonistsMolecular MedicineSpecific activityKetanserinSerotonin AntagonistsRadiopharmaceuticalsNuclear chemistry

description

Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparing the injectable [(18)F]MHMZ solution was 42% within a synthesis time of approximately 100 min. The novel compound showed excellent specific binding to the 5-HT(2A) receptor (K(i)=9.0 nM) in vitro and promising in vivo characteristics.

yearjournalcountryeditionlanguage
2007-11-05Bioorganicmedicinal chemistry letters
10.1016/j.bmcl.2007.12.054https://pubmed.ncbi.nlm.nih.gov/18187324