OAT3-Mediated Extrusion of the 99mTc-ECD Metabolite in the Mouse Brain. Issue 4 (April 2014)

• Record Type: Journal Article
• Authors: Kikuchi, Tatsuya; Okamura, Toshimitsu; Wakizaka, Hidekatsu; Okada, Maki; Odaka, Kenichi; Yui, Joji; Tsuji, Atsushi B; Fukumura, Toshimitsu; Zhang, Ming-Rong
• Is Part Of: Journal of cerebral blood flow & metabolism. Volume 34:Issue 4(2014)
• Page Start: 585
• Page End: 588
• Publication Date: 2014-04
• Subjects: blood–brain barrier -- brain imaging -- pharmacokinetics -- SPECT; Cerebral circulation -- Periodicals; Brain -- Metabolism -- Periodicals; Brain -- Blood-vessels -- Periodicals; Cerebrovascular disease -- Periodicals; 612.824
• DOI: 10.1038/jcbfm.2014.20
• Languages: English
• ISSNs: 0271-678X

Abstract

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.