Deutsch E, Libson K, Vanderheyden J L, Ketring A R, Maxon H R
Int J Rad Appl Instrum B. 1986;13(4):465-77. doi: 10.1016/0883-2897(86)90027-9.
The beta emitting isotopes 186Re and 188Re are logical choices on which to base therapeutic radiopharmaceuticals that might be expected to be analogous to diagnostic radiopharmaceuticals based on 99mTc. However, the chemistry of rhenium is sufficiently different from that of technetium so that the development of Re radiopharmaceuticals often cannot be predicated on the known chemistry and biological behavior of 99mTc radiopharmaceuticals. The relevant chemical differences involve the greater stability of the higher oxidation states of Re (and thus the greater tendency of reduced Re radiopharmaceuticals to undergo re-oxidation to perrhenate), and the greater substitution inertness of reduced Re complexes. These differences are illustrated in the preparation and use of 186Re (Sn)-HEDP and 99mTc(Sn)-HEDP diphosphonate radiopharmaceuticals designed, respectively, for palliative therapy and diagnosis of metastatic cancer to bone, and in the preparation and biodistribution of tr[186Re(DMPE)2Cl2]+ and [186Re(DMPE)3]+, analogs to the potential myocardial perfusion imaging agents tr-[99mTc(DMPE)2Cl2]+ and [99mTc(DMPE)3]+. [HEDP = (1-hydroxyethylidene)diphosphonate; DMPE = 1,2-bis(dimethylphosphino)ethane].
发射β射线的同位素186Re和188Re是制备治疗性放射性药物的合理选择,这类药物有望类似于基于99mTc的诊断性放射性药物。然而,铼的化学性质与锝有很大不同,因此铼放射性药物的研发往往不能基于99mTc放射性药物已知的化学和生物学行为。相关的化学差异包括铼的较高氧化态具有更高的稳定性(因此还原态的铼放射性药物更易再氧化为高铼酸盐),以及还原态铼配合物具有更大的取代惰性。这些差异体现在分别用于骨转移癌姑息治疗和诊断的186Re(Sn)-HEDP和99mTc(Sn)-HEDP二膦酸盐放射性药物的制备和使用中,也体现在tr[186Re(DMPE)2Cl2]+和[186Re(DMPE)3]+的制备和生物分布中,它们分别是潜在的心肌灌注显像剂tr-[99mTc(DMPE)2Cl2]+和[99mTc(DMPE)3]+的类似物。[HEDP = (1-羟基亚乙基)二膦酸盐;DMPE = 1,2-双(二甲基膦基)乙烷]