Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor.
Two novel triaryl ligands 2 and 5 with potent in vitro binding affinities for the cannabinoid subtype-2 (CB2) receptor were labeled with a positron-emitting radioactive nuclide (11)C. Radioligands [(11)C]2, [(11)C]5, and their analogs [(11)C]3 and [(11)C]4 were synthesized by O-[(11)C]methylation of their corresponding phenol precursors with [(11)C]CH(3)I. [(11)C]2-5 had relatively high uptakes (>1.2% injected dose/g tissue) in mouse brains.
Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
Masayuki
M
Fujinaga
Katsushi
K
Kumata
Kazuhiko
K
Yanamoto
Kazunori
K
Kawamura
Tomoteru
T
Yamasaki
Joji
J
Yui
Akiko
A
Hatori
Masanao
M
Ogawa
Yuichiro
Y
Yoshida
Nobuki
N
Nengaki
Jun
J
Maeda
Ming-Rong
MR
Zhang
D000818:Animals; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D001921:Brain / Q000000981:diagnostic imaging; D002250:Carbon Radioisotopes; D008024:Ligands; D051379:Mice; D049268:Positron-Emission Tomography; D011485:Protein Binding; D011859:Radiography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D043885:Receptor, Cannabinoid, CB2 / Q000378:metabolism*; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry
D001713:Biphenyl Compounds; D002250:Carbon Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D043885:Receptor, Cannabinoid, CB2; D013876:Thiophenes