Kloster G, Laufer P, Wutz W, Stöcklin G
Eur J Nucl Med. 1983;8(6):237-41. doi: 10.1007/BF00522512.
A number of D-glucose analogues labelled with either the positron emitter 75Br (T 1/2 = 1.6 h) or the single photon emitter 123I (T 1/2 = 13.3 h) were studied as potential tracers for glucose utilisation in heart and brain. Of these, 3-deoxy-3-bromo-D-glucose, 3-deoxy-3-iodo-D-glucose, methyl 2-deoxy-2-bromo-beta-D-glucoside and methyl 2-deoxy-2-iodo-beta-D-glucoside showed little uptake of radioactivity into brain and an unfavourable ratio of heart-to-blood and heart-to-lung concentrations. In contrast, methyl 3,4,6-tri-O-acetyl-2-deoxy-2-iodo-beta-D-glucoside (MTIG) and methyl 3,4,6-tri-O-acetyl-2-deoxy-2-bromo-beta-D-glucoside (MTBG) showed promising brain uptake (160% MBC for MTBG) with a good brain-to-blood concentration ratio of 0.8. MTBG is not metabolically altered in the brain. Thus, this compound may be a promising tracer for measuring glucose transport if it proves to be a substrate for the hexose carrier at the blood-brain-barrier.
人们研究了多种用正电子发射体(75Br)（半衰期(T_{1/2}=1.6)小时）或单光子发射体(123I)（半衰期(T_{1/2}=13.3)小时）标记的(D -)葡萄糖类似物，将其作为心脏和大脑中葡萄糖利用的潜在示踪剂。其中，(3 -)脱氧(-3 -)溴(-D -)葡萄糖、(3 -)脱氧(-3 -)碘(-D -)葡萄糖、甲基(2 -)脱氧(-2 -)溴(-β - D -)葡萄糖苷和甲基(2 -)脱氧(-2 -)碘(-β - D -)葡萄糖苷在大脑中的放射性摄取很少，且心脏与血液、心脏与肺部的浓度比不理想。相比之下，甲基(3,4,6 -)三(-O -)乙酰基(-2 -)脱氧(-2 -)碘(-β - D -)葡萄糖苷（MTIG）和甲基(3,4,6 -)三(-O -)乙酰基(-2 -)脱氧(-2 -)溴(-β - D -)葡萄糖苷（MTBG）在大脑中的摄取情况良好（MTBG为160%MBC），脑血浓度比为0.8。MTBG在大脑中不会发生代谢变化。因此，如果该化合物被证明是血脑屏障处己糖载体的底物，那么它可能是一种很有前景的用于测量葡萄糖转运的示踪剂。
