Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:19

Article

Donohue, Sean R.^1,2  Varnas, Katarina²  Jia, Zhisheng²  Gulyas, Balazs²  Pike, Victor W.¹  Halldin, Christer² 

[1] NIMH, Mol Imaging Branch, NIH, Bethesda, MD 20892 USA

[2] Karolinska Hosp, Karolinska Inst, Dept Clin Neurosci, Psychiat Sect, S-17176 Stockholm, Sweden

关键词: SPECT;    PET;    CB1 receptors;    Radioiodination;    Radioligand;   

DOI  :  10.1016/j.bmcl.2009.08.092

来源: Elsevier

【 摘 要 】

There is strong interest to study the involvement of brain cannabinoid subtype-1 (CB1) receptors in neuropsychiatric disorders with single photon emission computed tomography ( SPECT) and a suitable radioligand. Here we report the synthesis of a novel high-affinity radioiodinated CB1 receptor ligand ([I-125]8, [I-125]1-(2-iodophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxylate, [I-125] SD7015). By autoradiography in vitro, [I-125]8 showed selective binding to CB1 receptors on human brain postmortem cryosections and now merits labeling with iodine-123 for further evaluation as a SPECT radioligand in non-human primate. (c) 2009 Elsevier Ltd. All rights reserved.

【 授权许可】

Free