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The potential of o ‐bromo‐ trans ‐decalinvesamicol as a new PET ligand for vesicular acetylcholine transporter imaging
Author(s) -
Azim Mohammad Anwarul,
Kozaka Takashi,
Uno Izumi,
Miwa Daisuke,
Kitamura Yoji,
Ogawa Kazuma,
Makino Akira,
Kiyono Yasushi,
Shiba Kazuhiro
Publication year - 2014
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/syn.21756
Subject(s) - vesicular acetylcholine transporter , in vivo , ligand (biochemistry) , agonist , chemistry , acetylcholine , ex vivo , receptor , pentazocine , pharmacology , transporter , biochemistry , biology , in vitro , microbiology and biotechnology , morphine , gene , choline acetyltransferase
We investigated the characteristics of the regional rat brain distribution of radio‐brominated o ‐bromo‐decalinvesamicol (OBDV) in vivo to evaluate its potential as a PET ligand for vesicular acetylcholine transporter (VAChT). In in vivo biodistribution study, the specific brain regional accumulation of [ 77 Br]OBDV was revealed 30 min after intravenous injection. The specific brain regional accumulation of [ 77 Br]OBDV was significantly inhibited by co‐injection of (+/−)‐vesamicol. In contrast, no significant inhibition of the uptake of [ 77 Br]OBDV in all brain regions was observed with co‐injection of (+)‐pentazocine (selective σ‐1 receptor agonist) and (+)−3‐(3‐hydroxyphenyl)‐ N ‐propylpiperidine, [(+)−3‐PPP] (σ‐1 and σ‐2 receptor agonist) with [ 77 Br]OBDV. [ 77 Br]OBDV accumulation in VAChT‐rich brain regions was observed in ex vivo autoradiography. These results showed that [ 77 Br]OBDV selectively bound to VAChT with high affinity in rat brain in vivo . Hence, OVBDV radiolabelled with more suitable 76 Br was suggested to be a potent VAChT ligand for PET. Synapse 68:445–453, 2014 . © 2014 Wiley Periodicals, Inc.