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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetamides / chemical synthesis*
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Acetamides / pharmacology*
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Animals
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Autoradiography
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Binding, Competitive / drug effects
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Brain / diagnostic imaging
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Brain Chemistry / drug effects
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Central Nervous System / drug effects
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Central Nervous System / metabolism
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Electrons
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Flumazenil / metabolism
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Fluorine Radioisotopes
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GABA Modulators / metabolism
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In Vitro Techniques
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Mice
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Peripheral Nerves / drug effects*
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacology*
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Receptors, GABA-A / drug effects*
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Tomography, Emission-Computed
Substances
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Acetamides
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Fluorine Radioisotopes
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GABA Modulators
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N-(5-fluoro-2-phenoxyphenyl)-N-(2-fluoroethyl-5-methoxybenzyl)acetamide
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N-(5-fluoro-2-phenoxyphenyl)-N-(2-fluoromethyl-5-methoxybenzyl)acetamide
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Radiopharmaceuticals
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Receptors, GABA-A
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Flumazenil