Total synthesis and evaluation of [18F]MHMZ
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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.
Originalsprog | Engelsk |
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Tidsskrift | Bioorganic & Medicinal Chemistry Letters |
Vol/bind | 18 |
Udgave nummer | 4 |
Sider (fra-til) | 1515-1519 |
Antal sider | 5 |
ISSN | 0960-894X |
DOI | |
Status | Udgivet - 2008 |
ID: 14248300