title: [18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).
abstract: We synthesized and evaluated N-(5-fluoro-2-phenoxyphenyl)-N-(2-[(18)F]fluoromethyl-5-methoxybenzyl)acetamide ([(18)F]-FMDAA1106) and N-(5-fluoro-2-phenoxyphenyl)-N-(2-[(18)F]fluoroethyl-5-methoxybenzyl)acetamide ([(18)F]FEDAA1106) as two potent radioligands for peripheral benzodiazepine receptors (PBR). [(18)F]FMDAA1106 and [(18)F]FEDAA1106 were respectively synthesized by fluoroalkylation of the desmethyl precursor DAA1123 with [(18)F]FCH(2)I and [(18)F]FCH(2)CH(2)Br. Ex vivo autoradiograms of [(18)F]FMDAA1106 and [(18)F]FEDAA1106 binding sites in the rat brains revealed that a high radioactivity was present in the olfactory bulb, the highest PBR density region in the brain.
authors.affiliation: Department of Medical Imaging, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan. zhang@nirs.go.jp
authors.forename: Ming Rong
authors.initials: MR
authors.lastname: Zhang
authors.forename: Jun
authors.initials: J
authors.lastname: Maeda
authors.forename: Kenji
authors.initials: K
authors.lastname: Furutsuka
authors.forename: Yuichiro
authors.initials: Y
authors.lastname: Yoshida
authors.forename: Masanao
authors.initials: M
authors.lastname: Ogawa
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Suhara
authors.forename: Kazutoshi
authors.initials: K
authors.lastname: Suzuki
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000000981:diagnostic imaging; D001923:Brain Chemistry / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects / Q000378:metabolism; D004583:Electrons; D005442:Flumazenil / Q000378:metabolism; D005462:Fluorine Radioisotopes; D018757:GABA Modulators / Q000378:metabolism; D066298:In Vitro Techniques; D051379:Mice; D010525:Peripheral Nerves / Q000187:drug effects*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology*; D011963:Receptors, GABA-A / Q000187:drug effects*; D014055:Tomography, Emission-Computed
chemical_list: D000081:Acetamides; D005462:Fluorine Radioisotopes; D018757:GABA Modulators; C475621:N-(5-fluoro-2-phenoxyphenyl)-N-(2-fluoroethyl-5-methoxybenzyl)acetamide; C475620:N-(5-fluoro-2-phenoxyphenyl)-N-(2-fluoromethyl-5-methoxybenzyl)acetamide; D019275:Radiopharmaceuticals; D011963:Receptors, GABA-A; D005442:Flumazenil