Synthesis of a [6-pyridinyl-18 F]-labelled fluoro derivative of WAY-100635 as a candidate radioligand for brain 5-HT 1A receptor imaging with PET

…, C Hlavacek, F Vaufrey, C Halldin, JA McCarron…

Index: Karramkam, Mylene; Hinnen, Francoise; Berrehouma, Myriam; Hlavacek, Christophe; Vaufrey, Francoise; Halldin, Christer; McCarron, Julie A.; Pike, Victor W.; Dolle, Frederic Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 13 p. 2769 - 2782

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Citation Number: 52

Abstract

In recent years, considerable effort has been spent on the design, synthesis and pharmacological characterization of radiofluorinated derivatives of the 5-HT1A receptor antagonist, WAY-100635, for the in vivo study of these receptors in human brain with PET.(Pyridinyl-6)-fluoro-and (pyridinyl-5)-fluoro-analogues of WAY-100635 (6-fluoro and 5- fluoro-WAY-100635, 5a/6a) were synthesized as well as the corresponding chloro-, bromo ...