Synthesis of a [6-Pyridinyl-18F]-labelled fluoro derivative of WAY-100635 as a candidate radioligand for brain 5-HT1A receptor imaging with PET
✍ Scribed by Mylène Karramkam; Françoise Hinnen; Myriam Berrehouma; Christophe Hlavacek; Françoise Vaufrey; Christer Halldin; Julie A. McCarron; Victor W. Pike; Frédéric Dollé
- Book ID
- 108479350
- Publisher
- Elsevier Science
- Year
- 2003
- Tongue
- English
- Weight
- 393 KB
- Volume
- 11
- Category
- Article
- ISSN
- 0968-0896
No coin nor oath required. For personal study only.
📜 SIMILAR VOLUMES
## Abstract In this study, we synthesized and evaluated a new spirocyclic piperidine derivative 3, containing a 4‐fluorobutyl side chain, as a PET radioligand for neuroimaging of σ~1~ receptors. In vitro, compound 3 displayed high affinity for σ~1~ receptors (__K__~i~=1.2 nM) as well as high select
## Abstract 5‐HT~1A~ receptors are involved in a variety of psychiatric disorders and __in vivo__ molecular imaging of the 5‐HT~1A~ status represents an important approach to analyze and treat these disorders. We report herein the synthesis of three new fluoroethylated 5‐HT~1A~ ligands (AH1.MZ, AH2
## Abstract 4‐Fluoro‐__N__‐{2‐[4‐(6‐trifluoromethylpyridin‐2‐yl)piperazin‐1‐yl]ethyl}benzamide is a full 5‐HT~1A~ agonist with high affinity (__pK__~__i__~=9.3), selectivity and a __c__ log __P__ of 3.045. The corresponding PET radioligand 4‐[^18^F]fluoro‐__N__‐{2‐[4‐(6‐trifluoromethylpyridin‐2‐yl)