N-[3-[4-(2-methoxyphenyl) piperaziny-1-yl]propyl]cyclam: synthesized as a potential 5-HT1A receptor ligand and labelled with 99mTc-nitrido core

✍ Scribed by Fenglong Wang; Xuebin Wang; Shuye Yang; Jian Liu; Xianzhong Zhang

• Book ID: 102370727
• Publisher: John Wiley and Sons
• Year: 2008
• Tongue: French
• Weight: 130 KB
• Volume: 51
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.1532

✦ Synopsis

Abstract

This paper reports the synthesis of new potential 5‐HT~1A~ receptor ligand N‐[3‐[4‐(2‐methoxyphenyl)piperaziny‐1‐yl]propyl]cyclam (MPPC) and radiolabelling of it with ^99m^Tc‐nitrido core. The novel neutral complex ^99m^TcN‐MPPC combines 1,4,8,11‐tetraazacyclotetradecane (cyclam) ligand as chelate moiety for ^99m^Tc‐nitrido with a 1‐(2‐methoxyphenyl)piperazine moiety derived from WAY 100635 via a 3‐carbon alkyl chain. This provided a reliable and reproducible method for attaching the technetium to the pharmacophore moiety of WAY 100635. ^99m^TcN‐MPPC was prepared by a two‐step procedure and the radiochemical purity was found to be greater than 95%. It was hydrophilic and stable for at least 4 h at room temperature. In vivo stability study in normal rats showed that no degradation of ^99m^TcN‐MPPC was found in deproteinated blood samples at 2 h post‐injection. This effective ^99m^Tc‐labelling strategy for obtaining neutral ^99m^Tc nitrido complexes would be a useful tool to prepare new SPECT agents to image 5‐HT~1A~ receptor with cyclam conjugated ligands. Copyright © 2008 John Wiley & Sons, Ltd.