Hayes R L
Semin Nucl Med. 1978 Jul;8(3):183-91. doi: 10.1016/s0001-2998(78)80027-0.
The use of gallium radionuclides in nuclear medicine dates back to the late 1940s, following the observation in toxicologic studies that gallium tended to localize to a high degree at sites of osteogenic activity. Initial attempts in the early 1950s to use 72Ga for clinical diagnosis and therapy of malignant bone lesions were unproductive. However, the basic information gained then in the preclinical and clinical investigations was quite instrumental in generating the present-day use of gallium radionuclides as effective radiopharmaceutical agents. Although initial clinical trials of 72Ga were unproductive, subsequent studies with 68Ga and 67Ga, together with advances in nuclear medical instrumentation, resulted in the identification of gallium radionuclides as effective tumor- and abscess-localizing agents. A major factor in the recognition of the peculiar biologic properties of gallium radionuclides was the existence of a carrier (stable isotope) effect. Also, it appears from basic studies of the mechanism(s) of the uptake of gallium in tumor tissue that the biodistribution of gallium involves many essential biologic processes. The future use of gallium radionuclides may, therefore, actually very well fall more into the field of basic biologic investigations rather than into the field of nuclear medical diagnosis.
镓放射性核素在核医学中的应用可追溯到20世纪40年代末，当时毒理学研究观察到镓倾向于在成骨活性部位高度聚集。20世纪50年代初，使用72Ga对恶性骨病变进行临床诊断和治疗的初步尝试没有取得成果。然而，当时在临床前和临床研究中获得的基础信息对如今将镓放射性核素用作有效的放射性药物起到了很大作用。尽管72Ga的初步临床试验没有成效，但随后对68Ga和67Ga的研究，以及核医学仪器的进步，使得镓放射性核素被确定为有效的肿瘤和脓肿定位剂。认识镓放射性核素特殊生物学特性的一个主要因素是载体（稳定同位素）效应的存在。此外，从对镓在肿瘤组织中摄取机制的基础研究来看，镓的生物分布涉及许多重要的生物学过程。因此，镓放射性核素未来的应用实际上很可能更多地属于基础生物学研究领域，而不是核医学诊断领域。
