Changes in expression and dysfunctional signaling of TrkA/B/C receptors and oncogenic Trk fusion proteins are found in neurological diseases and cancers. Here, we describe the development of a first ¹⁸F-labeled optimized lead suitable for in vivo imaging of Trk, [¹⁸F]TRACK, which is radiosynthesized with ease from a nonactivated aryl precursor concurrently combining largely reduced P-gp liability and improved brain kinetics compared to previous leads while displaying high on-target affinity and human kinome selectivity.

中文翻译：

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鉴定[ ¹⁸ F] TRACK，一种18氟标记的Tropomyosin受体激酶（Trk）抑制剂，用于PET成像

在神经系统疾病和癌症中发现了TrkA / B / C受体和致癌性Trk融合蛋白的表达和功能异常信号的变化。在这里，我们描述了适用于Trk体内成像的第一个¹⁸ F标记的优化前导物[ ¹⁸ F] TRACK的开发，它可以轻松地由非活化的芳基前体进行放射合成，同时结合了大大降低的P-gp耐受性和改善的大脑与先前的导联相比，具有更高的动力学特性，同时展现出高的目标亲和力和人类kinome选择性。