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开发新型C-标记的选择性Orexin-2受体放射连接体,用于 pozitron发射断层成像

Jian Rong^1,2, Tomoteru Yamasaki³, Yinlong Li^1,2

¹Department of Radiology and Imaging Sciences, Emory University, Atlanta, Georgia 30322, United States.

ACS medicinal chemistry letters

|October 18, 2023

概括

研究人员开发了新型正子发射断层扫描 (PET) 配体[11C]OX2-2201和[11C]OX2-2202,用于在体内成像素2受体 (OX2R). 这些配体表现出高亲和力和选择性,但对大脑透需要进一步优化.

科学领域:

神经科学是一个神经科学.
放射化学放射化学是指辐射化学.
药理学药理学是指药理学的学科.

背景情况:

素2受体 (OX2R) 对于调节清醒和睡眠-清醒周期至关重要.
目前,对于OX2R.的体内成像,还没有正电子发射断层扫描 (PET) 标记剂.

研究的目的:

在体内开发和描述用于成像OX2R的新型PET配体.
评估新型标记物的结合亲和力,选择性和大脑吸收.

主要方法:

合成和放射性标记两种新型PET配体,即[11C]OX2-2201和[11C]OX2-2202.
在体外结合测试以确定亲和力 (Ki) 和选择性 (OX2/OX1比率).
在小鼠大脑中进行体外自发放射和体内PET成像,以评估结合特异性和大脑吸收.

主要成果:

[11C]OX2-2201和[11C]OX2-2202都表现出极好的结合亲和力 (Ki = 3.6 nM和2.2 nM,分别) 和对OX2R的高选择性 (OX2/OX1 > 600个折叠).
实验室自发放射学显示,在老鼠大脑中,结合特异性很好,甚至很好.
在体内PET成像显示,大脑对[11C]OX2-2202的吸收率较低,可能是由于流出输送器相互作用或低被动透性.

结论:

[11C]OX2-2201和[11C]OX2-2202是对OX2R具有高亲和力和选择性的有希望的新型PET配体.
需要进一步优化药物化学,以提高未来体内应用的脑透率.

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