Journal Article [11C]BCTC: Radiosynthesis and In Vivo Binding to Transient Receptor Potential Vanilloid Subfamily Member 1 (TRPV1) Receptor in the Mouse Trigeminal Nerve

Kumata, Katsushi  ,  Yui, Joji  ,  Zhang, Yiding  ,  Kurihara, Yusuke  ,  Ogawa, Masanao  ,  Mori, Wakana  ,  Fujinaga, Masayuki  ,  Ming-Rong, Zhang

27 ( 19 )  , pp.4521 - 4524 , 2017-09 , Elsevier
The purpose of this study was to synthesize a new positron emission tomography radiotracer, N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-[11C]carboxamide ([11C]BCTC, [11C]1), and assess its in vivo binding to the transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor in mice. [11C]BCTC was synthesized by reacting the hydrochloride of 4-tertiarybutylaniline (2•HCl) with [11C]phosgene ([11C]COCl2) to give isocyanate [11C]4, followed by reaction with 4-(3-chloropyridin-2-yl)tetrahydropyrazine (3). [11C]BCTC was obtained at a 16–20% radiochemical yield, based on the cyclotron-produced [11C]CO2 (decay-corrected to the end of bombardment), with > 98% radiochemical purity and 65–110 GBq/μmol specific activity at the end of synthesis. An ex vivo biodistribution study in mice confirmed the specific binding of [11C]BCTC to TRPV1 in the trigeminal nerve, which is a tissue with high TRPV1 expression.

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