Comparison of the binding of the irreversible monoamine oxidase tracers, [11C]clorgyline and [11C]l-deprenyl in brain and peripheral organs in humans

Comparison of the binding of the irreversible monoamine oxidase tracers, [11C]clorgyline and [11C]l-deprenyl in brain and peripheral organs in humans
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DOI:
10.1016/j.nucmedbio.2003.10.003
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发表时间:
2004-04-01
影响因子:
3.1
通讯作者:
Gatley, SJ
Gatley, SJ
中科院分区:
医学4区
文献类型:
--
作者:
Fowler, JS;Logan, J;Gatley, SJ

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比较了单胺氧合酶A和B(MAO A和13)放射性示踪剂[C-11]Clorgyline(CLG)和[C-11]L-丙稀基(DEP)与它们的氚标记对应物(CLG-D和DEP-D)在人体内的分布和动力学,以确定它们在人体内的分布和动力学是否与它们的物理、化学和药理性质以及已报道的死后组织中MAO A:MAO B的比例一致。DEP的不可逆结合在脑、心、肾和脾中持续较高,但在肺中不存在,在没有DEP结合的甲状腺中不存在。DEP结合率普遍较高与其较高的酶亲和力和血浆中较大的游离部分一致,而CLG和DEP在脑、心、甲状腺和肺中的区域分布差异与人MAO A和MAO B的不同相对比例相一致。由爱思唯尔公司出版。
The monoamine oxiclase A and B (MAO A and 13) radiotracers [C-11]clorgyline (CLG) and [C-11]L-deprenyl (DEP) and their deuterium labeled counterparts (CLG-D and DEP-D) were compared to determine whether their distribution and kinetics in humans are consistent with their physical, chemical and pharmacological properties and the reported ratios of MAO A:MAO B in post-mortem human tissues. Irreversible binding was consistently higher for DEP in brain, heart, kidneys and spleen but not lung where CLG >DEP and not in thyroid where there is no DEP binding. The generally higher DEP binding is consistent with its higher enzyme affinity and larger free fraction in plasma while differences in regional distribution for CLG and DEP in brain, heart, thyroid and lungs are consistent with different relative ratios of MAO A and B in humans. Published by Elsevier Inc.