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[ 11 C]BCTC: Radiosynthesis and in vivo binding to transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor in the mouse trigeminal nerve

[ 11 C]BCTC: Radiosynthesis and in vivo binding to transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor in the mouse trigeminal nerve

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

Bioorg Med Chem Lett. 2017 Oct 1;27(19):4521-4524.

PMID: 28888821

Abstract:

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 65-110GBq/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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP393514244	BCTC		393514-24-4	Price

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