Synthesis of [11C]RPR-72840A and its evaluation as a radioligand for the serotonin reuptake site in positron emission tomography.
RPR-72840A, an inhibitor of serotonin reuptake, was labelled with carbon-11. The synthesis of the nonradioactive precursor, which exhibited some unexpected chemistry, and its reaction with [11C]phosgene affording [11C]RPR-72840A are described. Biodistribution studies in rats and PET studies in baboons were conducted to evaluate [11C]RPR-72840A as a tracer for PET imaging of the serotonin reuptake system.
Roeda
D
D
CEA, Service Hospitalier Frédéric Joliot, Orsay, France. ROEDA@DSVIDF.CEA.FR
Tavitian
B
B
Coulon
C
C
David
F
F
Dollé
F
F
Fuseau
C
C
Jobert
A
A
Crouzel
C
C
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002250:Carbon Radioisotopes; D005069:Evaluation Studies as Topic; D008297:Male; D010215:Papio; D011799:Quinazolines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012701:Serotonin / Q000378:metabolism*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D011799:Quinazolines; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors; C105914:RPR 72840A