Synthesis of (+/-)-[18F]BMY 14802, its enantiomers and their anatomical distributions in rodents.
Nucl Med Biol
; 20(5): 625-30, 1993 Jul.
Article
en En
| MEDLINE
| ID: mdl-8358348
A potential antipsychotic drug, BMY 14802 was labeled with 18F and its distribution in rodents was studied. No-carrier-added (NCA) (+/-)-[18F]BMY 14802 (5) was synthesized by two methods in 5-10% radiochemical yield in a synthesis time of 130-140 min from EOB with a specific activity of 0.5-1.5 Ci/microM. (+)- and (-)-[18F]BMY 14802 was synthesized by the chiral reduction of alpha-(4-[18F]fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine-b utanone (4) with chiral reducing agent, (+)- and (-)-beta-chlorodiisopinocampheylborane [(+)- and (-)-DIP chloride] in 6-10% radiochemical yield in a synthesis time of 150 min from EOB. Animal studies in mouse and in rat revealed that the distribution of 5 in each tissue was high at 5 min, the radioactivity then declined rapidly in all tissues studied except in the liver and in the small intestine. The radioactivity in the femur did not increase with time indicating in vivo defluorination may not occur. The uptakes of (+/-)-[18F]BMY 14802 and its enantiomers, (+)- and (-)-[18F]BMY 14802 in rat cerebellum, brain stem, hippocampus and spinal cord were similar and were significantly reduced by prior treatment of rat with haldol. This suggests that (+/-)-[18F]BMY 14802 and its enantiomers bind to sigma-receptors in a similar fashion.
Buscar en Google
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirimidinas
Límite:
Animals
Idioma:
En
Revista:
Nucl Med Biol
Asunto de la revista:
BIOLOGIA
/
MEDICINA NUCLEAR
Año:
1993
Tipo del documento:
Article
Pais de publicación:
Estados Unidos