Fowler Joanna S, Logan Jean, Wang Gene-Jack, Volkow Nora D, Telang Frank, Ding Yu-Shin, Shea Colleen, Garza Victor, Xu Youwen, Li Zizhong, Alexoff David, Vaska Paul, Ferrieri Richard, Schlyer David, Zhu Wei, John Gatley S
Brookhaven National Laboratory, Chemistry Department, Bldg 555, Upton, NY 11973, USA.
Nucl Med Biol. 2004 Apr;31(3):313-9. doi: 10.1016/j.nucmedbio.2003.10.003.
The monoamine oxidase A and B (MAO A and B) radiotracers [(11)C]clorgyline (CLG) and [(11)C]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.
比较单胺氧化酶A和B（MAO A和B）放射性示踪剂[（11）C]氯吉兰（CLG）和[（11）C]L-司来吉兰（DEP）及其氘标记类似物（CLG-D和DEP-D），以确定它们在人体内的分布和动力学是否与其物理、化学和药理学特性以及死后人体组织中报道的MAO A:MAO B比率一致。DEP在脑、心脏、肾脏和脾脏中的不可逆结合始终较高，但在肺中CLG>DEP，而在甲状腺中则没有DEP结合。DEP通常较高的结合与其较高的酶亲和力和血浆中较大的游离分数一致，而CLG和DEP在脑、心脏、甲状腺和肺中的区域分布差异与人类MAO A和B的不同相对比率一致。
