title: The potential of o-bromo-trans-decalinvesamicol as a new PET ligand for vesicular acetylcholine transporter imaging.
abstract: 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.
authors: Division of Tracer Kinetics, Advanced Science Research Center, Kanazawa University, 13-1 Takara-machi, Kanazawa, Ishikawa, 920-8640, Japan; Graduate School of Natural Science and Technology, Kanazawa University, Kakuma, 920-1192, Japan.
authors: Mohammad Anwar-Ul
authors: MA
authors: Azim
authors: Takashi
authors: T
authors: Kozaka
authors: Izumi
authors: I
authors: Uno
authors: Daisuke
authors: D
authors: Miwa
authors: Yoji
authors: Y
authors: Kitamura
authors: Kazuma
authors: K
authors: Ogawa
authors: Akira
authors: A
authors: Makino
authors: Yasushi
authors: Y
authors: Kiyono
authors: Kazuhiro
authors: K
authors: Shiba
mesh_terms: D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000000981:diagnostic imaging* / Q000187:drug effects / Q000378:metabolism*; D001967:Bromine Radioisotopes / Q000493:pharmacokinetics; D002491:Central Nervous System Agents / Q000494:pharmacology; D008297:Male; D010423:Pentazocine / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D017207:Rats, Sprague-Dawley; D017480:Receptors, sigma / Q000819:agonists / Q000378:metabolism; D050494:Vesicular Acetylcholine Transport Proteins / Q000378:metabolism*
chemical_list: D001967:Bromine Radioisotopes; D002491:Central Nervous System Agents; D010880:Piperidines; D019275:Radiopharmaceuticals; D017480:Receptors, sigma; D050494:Vesicular Acetylcholine Transport Proteins; C578222:o-bromo-trans-decalinvesamicol; C006189:vesamicol; C026539:preclamol; D010423:Pentazocine
keywords: Alzheimer's disease.; PET ligand; Vesicular acetylcholine transporter; decalinvesamicol