Synthesis of [18F]fluoroalkylated analogues of a benzamide nuroleptic; YM-09151-2

✍ Scribed by Kentaro Hatano; Tastuo Ido; Kiichi Ishiwata; Koichiro Kawashiroa; Jun Hatazawa; Masatoshi Itoh; Ren Iwata

• Publisher: John Wiley and Sons
• Year: 1989
• Tongue: French
• Weight: 136 KB
• Volume: 26
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.25802601142

✦ Synopsis

Recently, i n vivo measurement of dopamine r e c e p t o r s i n human b r a i n u s i n g p o s i t r o n emission tomography (PET) w i t h a r a d i o l i g a n d l a b e l e d w i t h a p o s i t r o n emitter has been of g r e a t i n t e r e s r t .

W e p r e v i o u s l y proposed N-[(2RS,3RS)-l-benzyl-2-methyl-3-pyrrolidi-0 9 1 5 1 -1 ( u ) , a s t h e new and p o t e n t l i g a n d for t h e dopamine D2 r e c e p t o r measurements(1). YM-09151-2(ka) is r e p o r t e d t o be a dopamine a n t a g o n i s t t h a t has t h e high a f f i n i t y f o r D2 r e c e p t o r s which is s i m i l a r t o t h a t of s p i r o p e r i d o l , i n a d d i t i o n t o its good D2 s e l e c t i v i t y t h a t is t h e c h a r a c t e r i s t i c s of benzamide neurol e p t i c s . (2 )

The D2 s e l e c t i v i t y of C iiC]YM-09151-2 was a l s o determined i n v i v o .