PMID: 8971812Nov 29, 1996Paper

Ability of nitrobenzylthioinosine to cross the blood-brain barrier in rats

Neuroscience Letters
C M AndersonF E Parkinson

Abstract

Nucleoside transport inhibitors that cross the blood-brain barrier may be able to potentiate the neuroprotective effects of adenosine. We tested whether nitrobenzylthioinosine (NBMPR) crosses the blood-brain barrier in three types of experiments. First, intravenous injection of [3H]NBMPR and [14C]sucrose was performed. Brain volume of distribution and brain delivery were greater for [3H]NBMPR than for [14C]sucrose. Second, rats were injected intraperitoneally with NBMPR 5'-monophosphate (NBMPR-P), a prodrug form of NBMPR, or vehicle. Perchloric acid extracts of brains from rats treated with NBMPR-P inhibited [3H]NBMPR binding in competition binding assays nearly 3-fold more than extracts from brains of vehicle-treated animals. Third, cerebrospinal fluid (CSF) extracted from rats treated with NBMPR-P (10 mg/kg i.p.) contained 24.1 +/- 4.4 nM NBMPR while levels were undetectable in CSF from vehicle-treated rats. From these data, we conclude that NBMPR crosses the blood-brain barrier.

References

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Jan 1, 1997·Cancer Chemotherapy and Pharmacology·W P Gati, A R Paterson

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Citations

Mar 30, 2016·Pharmacology Research & Perspectives·Michael D NguyenB Jill Venton
Apr 15, 2005·Neurological Research·Fiona E ParkinsonChristina R Zamzow
Oct 4, 2000·Journal of Pharmaceutical Sciences·I Tamai, A Tsuji

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