Synthesis, characterization and biological evaluation of novel neutral fac-M(CO)₃(SNO) complexes (M=Re, ^99mTc) bearing the o-methoxyphenylpiperazine moiety

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• 作者：A. Chiotellis^a ; C. Tsoukalas^a ; ^{ctsoukal@rrp.demokritos.gr} ; M. Pelecanou^b ; I. Pirmettis^a ; M. Papadopoulos^a
• 关键词：Tricarbonyl Tc complexes ; 5-HT1A ; WAY-100635 ; Cysteine
• 刊名：Applied Radiation and Isotopes
• 出版年：2012
• 期刊代码：6_09698043
• 类别：ce
• 出版时间：June, 2012
• 卷：70
• 期：6
• 页码：957-964
• 文件大小：304 K

摘要

The synthesis, characterization and biological evaluation of two new neutral tricarbonyl fac-M(CO)₃(SNO) (M=Re, ^99mTc) bearing o-methoxyphenylpiperazine as pharmacophore and S-functionalized cysteine or penicillamine as chelators are reported. Competition binding tests showed good affinity for the 5-HT_1A receptor (8 and 54 nM for 4a and 4b, respectively). Biodistribution studies in healthy animals showed high initial blood and liver uptake, fast blood and tissue depuration and negligible brain uptake.