Development of probes and methods for noninvasive and quantitative assessment of efflux systems in the brain

开发用于无创和定量评估大脑流出系统的探针和方法

• 批准号: 20790920
• 负责人: OKAMURA Toshimitsu
• 金额: $ 2.66万
• 依托单位: National Institute of Radiological Sciences
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (B)
• 财政年份: 2008
• 资助国家: 日本
• 起止时间: 2008 至 2009
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-20790920/
• 关键词: 放射性医薬品; PET薬剤; グルタチオン抱合体; 異物排出トランスポータ; プリン

The aim of this study is to develop radioactive probes for noninvasive and quantitative measurement of brain efflux systems. The novel probe readily enters the brain and is converted to its glutathione conjugate, which is specifically transported by an efflux transporter MRP1. The probe can measure brain efflux systems noninvasively and quantitatively.

本研究的目的是开发用于脑外排系统无创定量测量的放射性探针。这种新型探针很容易进入大脑，并被转化为谷胱甘肽缀合物，由外排转运蛋白MRP1特异性运输。该探头可以无创、定量地测量脑外排系统。

项目成果

6-Bromo-7-[11C]- methylpurine is a Specific Probe for the ABC Transporter Mrp1, but not for Mrp2, Pgp, and Bcrp

6-Bromo-7-[11C]-methylpurine 是 ABC 转运蛋白 Mrp1 的特异性探针，但不适用于 Mrp2、Pgp 和 Bcrp

• 发表时间: 2009
• 作者: Okamura;T.;et;al.
• 通讯作者: al.

Noninvasive and quantitative assessment of the function of multidrug resistance-associated protein 1 in the living brain

• DOI: 10.1038/jcbfm.2008.135
• 发表时间: 2009-03-01
• 期刊: JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
• 影响因子: 6.3
• 作者: Okamura, Toshimitsu;Kikuchi, Tatsuya;Irie, Toshiaki
• 通讯作者: Irie, Toshiaki

Reactivity of 6-Halopurine Analogs with Glutathione as a Radiotracer for Assessing Function of Multidrug Resistance-Associated Protein 1

• DOI: 10.1021/jm901332c
• 发表时间: 2009-11-26
• 期刊: JOURNAL OF MEDICINAL CHEMISTRY
• 影响因子: 7.3
• 作者: Okamura, Toshimitsu;Kikuchi, Tatsuya;Irie, Toshiaki
• 通讯作者: Irie, Toshiaki

A PET Probe for Quantitatively Assessing the Efflux Transport Function of Multidrug Resistance-Associated Protein 1 in the Brain

用于定量评估大脑中多药耐药相关蛋白 1 的外排转运功能的 PET 探针

• 发表时间: 2008
• 作者: Okamura;T.;et;al.
• 通讯作者: al.

Evaluation of the conversion rate of 6-halogenopurine derivatives as a probe for assessing mrpl function

评估 6-卤代嘌呤衍生物的转化率作为评估 mrpl 功能的探针

• 发表时间: 2009
• 作者: Okamura;T.;et;al.
• 通讯作者: al.