Transferrin and transferrin receptors play an important role in the tr
ansport of iron into the brain, To determine whether gallium enters th
e brain by the same mechanism, uptakes of Ga-67 and Fe-59 have been co
mpared under controlled conditions, Rates of gallium penetration into
brain (K-in) were four times slower than those for Fe-59, K-in for Ga-
67 when infused with citrate were 0.88+/-0.24 and 0.94+/-0.39x10(-3) m
l g(-1)h(-1) for cerebral hemisphere and cerebellum, respectively, Whe
n infused as the transferrin complex, Ga-67 uptake into the brain was
not different from that when infused with citrate, The presence of the
anti-transferrin receptor antibody OX-26 significantly reduced uptake
of Fe-59 by 60% and 64% into cerebral hemisphere and cerebellum, resp
ectively., By contrast, pretreatment of rats with OX-26 enhanced the u
ptake of Ga-67 into brain, particularly when infused with citrate; mea
n increases in uptake of Ga-67 were 120% and 144% for cerebral hemisph
ere and cerebellum, respectively, Purified Ga-67-transferrin was also
taken up into both brain regions examined in the presence of OX-26, Th
ese results indicate that the transport of non-transferrin bound galli
um is an important mechanism for gallium uptake into brain.