PREPARATION OF [F-18] RP-62203, A SELECTIVE LIGAND FOR THE STUDY OF SEROTONIN RECEPTORS (5-HT2) BY RAPID IN-SITU PIPERAZINE FORMATION

Authors
LASNE MC BARRE L HUARD C LESECQ B COLLINS M
Citation
Mc. Lasne et al., PREPARATION OF [F-18] RP-62203, A SELECTIVE LIGAND FOR THE STUDY OF SEROTONIN RECEPTORS (5-HT2) BY RAPID IN-SITU PIPERAZINE FORMATION, Applied radiation and isotopes, 45(11), 1994, pp. 1085-1091
Citations number
27
Categorie Soggetti
Nuclear Sciences & Tecnology","Radiology,Nuclear Medicine & Medical Imaging
Journal title
Applied radiation and isotopes
ISSN journal
09698043 → ACNP
Volume
45
Issue
11
Year of publication
1994
Pages
1085 - 1091
Database
ISI
SICI code
0969-8043(1994)45:11<1085:PO[RAS>2.0.ZU;2-Y
Abstract
)propyl]-2H-naphth[1,8-cd]isothiazole-1,1-dioxide] ([F-18]RP 62203), a n antagonist of 5-HT2 receptors, was prepared from [F-18]fluoride via a 3-step reaction sequence, with an overall radiochemical yield of 5-1 2% (decay corrected) and within 190-230 min (total automated synthesis from EOB). The key step involved the rapid (6 min, 150 degrees C in o ctanol) and efficient (> 65%) reaction of an appropriate bis(bromoethy l)amine derivative with 4-[F-18]fluoroaniline.