Total synthesis and evaluation of [18F]MHMZ
Research output: Contribution to journal › Journal article › Research › peer-review
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.
| Original language | English |
|---|---|
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Volume | 18 |
| Issue number | 4 |
| Pages (from-to) | 1515-1519 |
| Number of pages | 5 |
| ISSN | 0960-894X |
| DOIs | |
| Publication status | Published - 2008 |
- Animals, Binding, Competitive, Brain, Fluorine Radioisotopes, Fluorobenzenes, Isotope Labeling, Ketanserin, Kinetics, Piperidines, Radioligand Assay, Radiopharmaceuticals, Rats, Receptor, Serotonin, 5-HT2A, Serotonin 5-HT2 Receptor Antagonists, Serotonin Antagonists
Research areas
ID: 14248300