Synthesis and evaluation of fluorinated derivatives of fentanyl as candidates for opiate receptor studies using positron emission tomograpry

✍ Scribed by Dah-Ren Hwang; Anthony L. Feliu; Alfred P. Wolf; Robert R. Macgregor; Joanna S. Fowler; Carroll D. Amett; H. Jean Holland; Kenneth Carr; Eric J. Simon

• Book ID: 102901068
• Publisher: John Wiley and Sons
• Year: 1986
• Tongue: French
• Weight: 619 KB
• Volume: 23
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580230306

✦ Synopsis

with [3H]naltrexona f o r binding sites i n rat b r a i n membranes. Both f e n t a n y l a n d h e x h i b i t e d a similar high "sodium r a t i o " (quotient of t h e IC50's a g a i n s t [3H]naltrexone i n t h e presence and absence of sodium c h l o r i d e ) g e n e r a l l y c h a r a c t e r i s t i c of o p i a t e a g o n i s t s . The a n a l g e s i c p o t e n c i e s of f e n t a n y l a n d a w e r e determined i n r a t s by measuring suppression of locomotion and v o c a l i z a t i o n responses t o footshock. 4 appeared s l i g h t l y less potent than f e n t a n y l , but produced a s i m i l a r a n a l g e s i a and c a t a l e p s y which was e n t i r e l y blocked by pretreatment of rats with naloxone, an o p i a t e a n t a g o n i s t . A ra i d s y n t h e s i s of [18F]-determined 5 , 60, and 120 minutes a f t e r intravenous i n j e c t i o n .