1299458-91-5Relevant articles and documents
Neopentyl Glycol as a Scaffold to Provide Radiohalogenated Theranostic Pairs of High in Vivo Stability
Arano, Yasushi,Hatazawa, Jun,Ishioka, Noriko S.,Kaizuka, Yuta,Ooe, Kazuhiro,Sasaki, Ichiro,Shirakami, Yoshifumi,Suzuki, Hiroyuki,Tanaka, Hiroshi,Tatsuta, Maho,Teramoto, Takahiro,Toyoshima, Atsushi,Uehara, Tomoya,Washiya, Nana,Watabe, Tadashi,Watanabe, Shigeki
, p. 15846 - 15857 (2021/11/16)
The high in vivo stability of 2,2-dihydroxymethyl-3-[18F]fluoropropyl-2-nitroimidazole ([18F]DiFA) prompted us to evaluate neopentyl as a scaffold to prepare a radiotheranostic system with radioiodine and astatine. Three DiFA analogues with one, two, or without a hydroxyl group were synthesized. While all 125I-labeled compounds remained stable against nucleophilic substitution, only a 125I-labeled neopentyl glycol was stable against cytochrome P450 (CYP)-mediated metabolism and showed high stability against in vivo deiodination. 211At-labeled neopentyl glycol also remained stable against both nucleophilic substitution and CYP-mediated metabolism. 211At-labeled neopentyl glycol showed the biodistribution profiles similar to those of its radioiodinated counterpart in contrast to the 125I/211At-labeled benzoate pair. The urine analyses confirmed that 211At-labeled neopentyl glycol was excreted in the urine as a glucuronide conjugate with the absence of free [211At]At-. These findings indicate that neopentyl glycol would constitute a promising scaffold to prepare a radiotheranostic system with radioiodine and 211At.
