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HBED:一种用于铁螯合治疗的去铁胺潜在替代物。

HBED: A potential alternative to deferoxamine for iron-chelating therapy.

作者信息

Bergeron R J, Wiegand J, Brittenham G M

机构信息

Department of Medicinal Chemistry, University of Florida, Gainesville, FL 32610, USA.

出版信息

Blood. 1998 Feb 15;91(4):1446-52.

PMID:9454776
Abstract

To examine the potential clinical usefulness of the hexadentate phenolic aminocarboxylate iron chelator N, N-bis(2-hydroxybenzyl)ethylenediamine-N,N-diacetic acid (HBED) for the chronic treatment of transfusional iron overload, we compared the iron excretion induced by subcutaneous (SC) injection of HBED and deferoxamine (DFO), the reference chelator, in rodents and primates. In the non-iron-overloaded, bile-duct-cannulated rat, a single SC injection of HBED, 150 micromol/kg, resulted in a net iron excretion that was more than threefold greater than that after the same dose of DFO. In the iron-loaded Cebus apella monkey, a single SC injection of HBED, 150 micromol/kg, produced a net iron excretion that was more than twice that observed after the same dose of SC DFO. In patients with transfusional iron overload, SC injections of HBED may provide a much needed alternative to the use of prolonged parenteral infusions of DFO.

摘要

为了研究六齿酚氨基羧酸盐铁螯合剂N,N-双(2-羟基苄基)乙二胺-N,N-二乙酸(HBED)对输血性铁过载进行长期治疗的潜在临床实用性,我们比较了皮下注射HBED和参比螯合剂去铁胺(DFO)在啮齿动物和灵长类动物中诱导的铁排泄情况。在未发生铁过载且胆管插管的大鼠中,皮下注射150微摩尔/千克的HBED,其净铁排泄量比相同剂量的DFO注射后的净铁排泄量高三倍多。在铁过载的僧帽猴中,皮下注射150微摩尔/千克的HBED,其净铁排泄量比相同剂量皮下注射DFO后观察到的净铁排泄量高出两倍多。对于输血性铁过载患者,皮下注射HBED可能为长期胃肠外输注DFO提供急需的替代方法。

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