75, 77Br- and 123I-analogues of d-glucose as potential tracers for glucose utilisation in heart and brain

Abstract

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.

A critical survey of experimental cross section data, comparison with nuclear model calculations and estimation of production yields of 77Br and 77Kr in no-carrier-added form via various nuclear processes

“…In general, reactions induced by all the light charged particles, viz. p, d, 3 He and a particles, have been investigated; in practice, however, the proton and a-particle induced reactions have been commonly employed. Some of the nuclear processes have been extensively studied while in several other cases the database is rather weak.…”

“…proton, deuteron, 3 He, and a-particle induced processes, in the same way as described by us earlier for protons on selenium [16]. The code ALICE was originally developed by Blann in 1975 and modified to ALICE-91 [33] which is based on the hybrid, the geometry-dependent hybrid (GDH) or the hybrid Monte Carlo simulation (HMS) pre-equilibrium models, and the Weisskop-Ewing evaporation formalism.…”

“…The neutron deficient radioisotopes of bromine have found some use in nuclear medicine, mainly due to a chemical behavior which is conducive to the synthesis of radiopharmacuticals [1][2][3][4][5][6]. Of all bromine radioisotopes the properties of 77 Br (T 1/2 = 56 h) are very suitable for in vivo studies.…”

“…Several groups around the world in general, and the Jülich group in Germany, in particular, have been considerably interested in investigating the production of bromine radioisotopes via p-, d-, 3 He-and a-particle induced reactions on several target materials (for reviews cf. [14,15]).…”

Nuclear Imaging of Glucose Transport/Metabolism – An Interesting Tool to Screen Insulin Resistance, Refine Diagnosis of Type 2 Diabetes, Understand Disease Mechanisms, and/or Evaluate New Therapies

“…Given the significant interest of a tracer to estimate alterations of glucose uptake in vivo, numerous researchers have tried for many years to develop glucose molecules labelled with a radioactive atom which is a pure -emitter, such as iodine 123, and which could be used routinely in Single Photon Emission Computed Tomography (SPECT), in all Nuclear Medicine centers (Kloster et al, 1983a(Kloster et al, , 1983bGoodman et al, 1981aGoodman et al, , 1981bLutz et al, 1991;Magata et al, 1992;Koumanov et al, 1997aKoumanov et al, , 1997bPerret et al, 2004). [ 123 I]-6-deoxy-6-iodo-D-glucose (6DIG) was first synthetized by Wassenar and colleagues, but the biological evaluation was limited to tumor uptake and not evaluated further (Wassenaar et al, 1973).…”