α₁-Adrenoceptor is implicated in numerous neuronal diseases. The development of new modulators targeting this receptor as well as the investigation of the role of α₁-adrenoceptor in healthy and disease conditions, however, is hindered by the lack of specific positron emission tomography (PET) radiotracers. Iloperidone shows a high binding affinity to α₁-adrenoceptor and moderate selectivity over other brain receptors. We report herein the synthesis and characterization of carbon-11 labeled iloperidone for imaging of α₁-adrenoceptor in brain. The radiolabeling of [¹¹C]iloperidone was carried out conveniently in one step by treating precursor with [¹¹C]CH₃I in DMF in the presence of K₂CO₃. Then, [¹¹C]iloperidone was purified by semi-preparative HPLC, and characterized in C57BL/6 mice using PET/CT scanning. The desired product [¹¹C]iloperidone was obtained in an average decay corrected radiochemical of 12% (n = 3) and over 99% radiochemical purity. The average molar radioactivity was 357 GBq/μmol with total synthetic time of 35–40 min. PET/CT scanning in C57BL/6 mice showed favorable pharmacokinetic properties and high brain exposure of [¹¹C]iloperidone. Blocking experiments by pretreatment with the unlabeled iloperidone showed the significant blocking effects with about 25% reduction in brain uptake. These results suggested that [¹¹C]iloperidone can serve as a lead compound for the further development of specific radiotracers for PET imaging of α₁-adrenoceptor in brain clinically.

α ₁ -肾上腺素能受体在许多神经元疾病有关。新的调制器针对这种受体的发展以及α的作用的调查_1种在健康和疾病情况肾上腺素受体，然而，由于缺乏具体的正电子发射断层扫描（PET）示踪剂的阻碍。伊潘立酮示出了高结合亲和力的α ₁ -肾上腺素能受体和适度选择性超过其它脑受体。我们在此报告碳-11标记的伊潘立酮的合成和表征为α成像₁在脑-肾上腺素能受体。通过[ ¹¹ C] CH ₃处理前体可以方便地一步一步进行[ ¹¹ C]哌啶酮的放射性标记I在DMF中K ₂ CO ₃的存在下。然后，通过半制备型HPLC纯化[ ¹¹ C]哌啶酮，并使用PET / CT扫描在C57BL / 6小鼠中进行鉴定。获得的所需产物[ ¹¹ C]哌啶酮的平均衰变校正放射化学值为12％（ñ= 3）和超过99％的放射化学纯度。平均摩尔放射性为357 GBq /μmol，总合成时间为35-40分钟。在C57BL / 6小鼠中进行PET / CT扫描显示出良好的药代动力学特性和[ ¹¹ C]哌拉啶酮的高脑暴露。通过用未标记的伊潘立酮进行预处理的阻断实验显示了显着的阻断作用，使大脑摄取降低了约25％。这些结果表明，[ ¹¹ C]伊潘立酮可以作为特定放射性示踪剂的进一步发展为α的PET成像铅化合物₁在脑-肾上腺素受体的临床情况。