OAT3-mediated extrusion of the 99mTc-ECD metabolite in the mouse brain.
After administration of the (99m)Tc complex with N,N'-1,2-ethylenediylbis-L-cysteine diethyl ester ((99m)Tc-ECD), a brain perfusion imaging agent, the radioactive metabolite is trapped in primate brain, but not in mouse and rat. Here, we investigate the involvement of metabolite extrusion by organic anion transporter 3 (OAT3), which is highly expressed at the blood-brain barrier in mice, in this species difference. The efflux rate of radioactivity in the cerebrum of Oat3(-/-) mice at later phase was 20% of that of control mice. Thus, organic anion transporters in mouse brain would be involved in the low brain retention of radioactivity after (99m)Tc-ECD administration.
Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Tatsuya
T
Kikuchi
Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Toshimitsu
T
Okamura
Biophysics Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Hidekatsu
H
Wakizaka
Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Maki
M
Okada
Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Kenichi
K
Odaka
Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Joji
J
Yui
Diagnostic Imaging Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Atsushi B
AB
Tsuji
Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Toshimitsu
T
Fukumura
Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan.
Ming-Rong
MR
Zhang
D000818:Animals; D001812:Blood-Brain Barrier / Q000000981:diagnostic imaging / Q000378:metabolism*; D054022:Cerebrum / Q000000981:diagnostic imaging / Q000378:metabolism*; D003545:Cysteine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D018345:Mice, Knockout; D029362:Organic Anion Transporters, Sodium-Independent / Q000235:genetics / Q000502:physiology*; D015609:Organotechnetium Compounds / Q000378:metabolism* / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000378:metabolism* / Q000493:pharmacokinetics; D015899:Tomography, Emission-Computed, Single-Photon
D029362:Organic Anion Transporters, Sodium-Independent; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C114338:organic anion transport protein 3; C059659:technetium Tc 99m bicisate; D003545:Cysteine