Dissemin is shutting down on January 1st, 2025

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Elsevier, Bioorganic and Medicinal Chemistry Letters, 16(23), p. 4567-4570

DOI: 10.1016/j.bmcl.2013.06.025

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Synthesis and in vitro cellular uptake of 11C-labeled 5-aminolevulinic acid derivative to estimate the induced cellular accumulation of protoporphyrin IX

Journal article published in 2013 by Chie Suzuki, Koichi Kato, Atsushi B. Tsuji ORCID, Tatsuya Kikuchi, Ming-Rong Zhang, Yasushi Arano, Tsuneo Saga
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

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Abstract

Protoporphyrin IX (PpIX) accumulation induced by exogenous 5-aminolevulinic acid (ALA) in tumors affects the therapeutic efficacy of ALA-based photodynamic and sonodynamic therapies. To develop a new imaging probe to estimate the ALA-induced PpIX accumulation, (11)C-labeled ALA analog (4), an ALA-dehydratase inhibitor, was radiosynthesized via (11)C-methylation of a Schiff-base-activated precursor in the presence of tetrabutylammonium fluoride, followed by the hydrolysis of ester and imine groups. The cellular uptake of 4 linearly increased with time and was inhibited by ALA and other transporter competitors. Monitoring analog 4 with positron emission tomography might be useful to estimate the ALA-induced PpIX accumulation in tumors.