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Pet imaging studies of dopamine D 2 receptors: Comparison of [ 18 F]N‐Methylspiperone; and the benzamide analogues [ 18 F]MABN and [ 18 F]MBP in baboon brain
Author(s) -
Mach Robert H.,
Ehrenkaufer Richard L. E.,
Greenberg Joel H.,
Shao Lingxiong,
Morton Thomas E.,
Evora Paul H.,
Nowak Peggy A.,
Luedtke Robert R.,
Cohen David,
Reivich Martin
Publication year - 1995
Publication title -
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Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/syn.890190305
Subject(s) - benzamide , chemistry , stereochemistry , in vivo , receptor , biochemistry , biology , microbiology and biotechnology
A series of positron emission tomography (PET) imaging studies was conducted in a baboon with the benzamide derivatives [ 18 F]2,3‐dimethoxy N‐9‐(4‐fluorobenzyl)‐9‐azabicyclo[3.3.1]nonan‐3β‐yl]benzamide ([ 18 F]MABN) and [ 18 F]2,3‐dimethoxy‐ N ‐[1‐(4‐fluorobenzyl)piperidin‐4‐yl]benzamide ([ 18 F]MBP). Studies were also conducted with the butyrophenone [ 18 F]N‐methylspiperone (NMSP) for comparison. Tissue‐time activity curves of [ 18 F]MABN are similar to those of [ 18 F]NMSP since both compounds displayed approximately the same uptake in the basal ganglia and displayed irreversible binding kinetics in vivo. However, the rapid rate of clearance from the cerebellum and high basal ganglia: cerebellum ratio of [ 18 F]MABN indicate that this compound has a much lower amount of nonspecific binding than [ 18 F]NMSP. [ 18 F]MBP displayed a higher uptake in the basal ganglia relative to [ 18 F]NMSP and [ 18 F]MABN and exhibited reversible binding kinetics in vivo. This property of [ 18 F]MBP is desirable since the uptake of radioactivity in D 2 ‐rich ligands is less likely to be influenced by changes in cerebral blood flow. The current data suggest that both [ 18 F]MABN and [ 18 F]MBP are promising ligands for studying dopamine D 2 receptors with PET. © 1995 Wiley‐Liss, Inc.