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在结构指导下发现了与素受体结合的PET连接体

Katharina Distler¹, Simone Maschauer², Eduard Neu¹

¹Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany; FAU NeW - Research Center New Bioactive Compounds, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.

Bioorganic & medicinal chemistry

|July 4, 2024

概括

研究人员开发了两种新的正电子发射断层扫描 (PET) 放射性连接体,即[18F]KD23和[18F]KD10,用于成像大脑素受体. 这些化合物提供了对素系统的更好的理解.

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:

素系统在调节生理和病理生理过程中起着至关重要的作用.
了解素受体 (OX1R和OX2R) 的表达和体内成像是至关重要的.
定子发射断层扫描 (PET) 是用于大脑分子成像的强大工具.

研究的目的:

使用PET设计和合成用于可视化素受体的新型放射性链体.
为OX1R和OX2R开发亚型选择性成像剂.
推进研究素系统在各种条件下的参与.

主要方法:

设计和合成由晶体结构指导的新型放射性连接体 ([18F]KD23和[18F]KD10).
用基基替换三醇部分的生物异构替代,以进行结构修改.
皮纳科尔前体的放射性标记,以获得最终的放射性连接体.

主要成果:

[18F]KD23对OX1R表现出高亲和力和对OX2R的选择性.
[18F]KD10对OX1R和OX2R亚型都表现出很高的亲和力.
在20分钟内获得了优异的放射化学产量 (93%的[18F]KD23,88%的[18F]KD10).

结论:

新型放射性连体[18F]KD23和[18F]KD10适用于PET研究.
这些化合物将促进大脑组织中素受体的亚型选择性成像.
开发的放射性连体将增强我们对素系统的理解.

关键词:

(18) F标签的使用.G蛋白结合受体的受体是G蛋白结合受体的受体.素受体的受体是什么?在PET中,PET连接物是PET连接物.

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