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

被引：7

作者：

Chiotellis, A. ^{[1
]}

Tsoukalas, C. ^{[1
]}

Pelecanou, M. ^{[2
]}

Pirmettis, I. ^{[1
]}

Papadopoulos, M. ^{[1
]}

机构：

[1] Natl Ctr Sci Res Demokritos, Inst Radioisotopes, Athens 15310, Greece

[2] Natl Ctr Sci Res Demokritos, Inst Biol, Athens 15310, Greece

来源：

APPLIED RADIATION AND ISOTOPES | 2012年 / 70卷 / 06期

关键词：

Tricarbonyl Tc complexes; 5-HT1A; WAY-100635; Cysteine; BRAIN 5-HT1A RECEPTORS; IN-VIVO; TRICARBONYL COMPLEXES; ORGANOMETALLIC TECHNETIUM; IMAGING AGENTS; HIGH-AFFINITY; LIGANDS; RADIOLIGAND; ANALOGS; RE;

D O I：

10.1016/j.apradiso.2012.03.003

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

The synthesis, characterization and biological evaluation of two new neutral tricarbonyl fac-M(CO)(3)(SNO) (M=Re, Tc-99m) bearing o-methoxyphenylpiperazine as pharmacophore and S-functionalized cysteine or penicillamine as chelators are reported. Competition binding tests showed good affinity for the 5-HT1A 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 deputation and negligible brain uptake. (c) 2012 Elsevier Ltd. All rights reserved.

引用

页码：957 / 964

页数：8

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