New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET.
A series of fluorinated diphenylchalcogen derivatives, possessing a sulfur or an oxygen bridge, has been prepared with the aim to get a suitable radiotracer to image the SERT in vivo using positron emission tomography (PET). The compounds were synthesized and assayed toward the serotonin (SERT), dopamine (DAT), and norepinephrine (NET) transporters. Among the developed series, five compounds display a high SERT affinity (K(i): 0.27-2.91 nM range) and can be labeled either with carbon-11 or fluorine-18.
Institut für Interdisziplinäre Isotopenforschung, Permoserstr 15, 04318, Leipzig, Germany. vercouillie@univ-tours.fr
Johnny
J
Vercouillie
Winnie
W
Deuther-Conrad
Matthias
M
Scheunemann
Patrick
P
Emond
Steffen
S
Fischer
Uta
U
Funke
Jörg
J
Steinbach
Denis
D
Guilloteau
Peter
P
Brust
D000818:Animals; D001921:Brain / Q000187:drug effects; D018011:Chalcogens / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004298:Dopamine / Q000378:metabolism; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008956:Models, Chemical; D009638:Norepinephrine / Q000378:metabolism; D049268:Positron-Emission Tomography / Q000379:methods*; D051381:Rats; D012701:Serotonin / Q000378:metabolism; D050486:Serotonin Plasma Membrane Transport Proteins / Q000737:chemistry*; D015398:Signal Transduction
D018011:Chalcogens; D006845:Hydrocarbons, Fluorinated; D050486:Serotonin Plasma Membrane Transport Proteins; D012701:Serotonin; D004298:Dopamine; D009638:Norepinephrine