应用于GABA_(A)型受体激动剂体外活性筛选的新型荧光染料合成及其方法构建  

Applied in the GABA_(A) Receptor Agonist Activity in Vitro Screening of New Fluorescent Dye Synthesis and its Construction Method

作　　者：徐小军 付岩 虞贤浩 周双林 胡英 常永昌 Xu Xiaojun;Fu Yan;Yu Xianhao;Zhou Shuanglin;Hu Ying;Chang Yongchang(Pharmaceutical Engineering Institute,Zhejiang Pharmaceutical College,Ningbo 315100;Agricultural Products Quality Inspection Center,Ningbo Academy of Agricultural Sciences,Ningbo 315040;Barrow Neurological Institute,St Joseph’s Hospital and Medical Center,Phoenix,AZ 85013,USA)

机构地区：[1]浙江药科职业大学制药工程学院,浙江宁波315100 [2]宁波市农业科学研究院农产品质量检测中心,浙江宁波315040 [3]Barrow Neurological Institute,St Joseph’s Hospital and Medical Center,Phoenix,AZ 85013,USA

出　　处：《广东化工》2022年第8期1-3,12,共4页Guangdong Chemical Industry

基　　金：浙江省自然科学基金基础公益研究计划项目(LGF21H180012);宁波市自然科学基金项目(2019A610190);校级重点科研课题(XZ2020001)。

摘　　要：氨基丁酸A型受体(GABA_(A)R)是γ-氨基丁酸门控的氯离子通道,针对该受体激动剂的体外活性筛选依赖于设备昂贵、操作要求高且效率低的电压钳技术,为此本课题合成得到一个新荧光染料C4,用γ-氨基丁酸作为激动剂,构建荧光法α1β2γ2γ-氨基丁酸受体激动剂的体外活性筛选方法,经研究表明当荧光染料C4浓度选用100μM时,能准确筛选激动剂γ-氨基丁酸的体外活性并计算得到其EC_(50)值(29.44±7.45μM),与通过电压钳技术筛选得到的EC_(50)值非常接近,达到高通量、快速、操作简便、设备要求低、精确筛选的要求,同时为其他神经受体激动剂体外活性筛选提供理论依据和技术支持。The γ-aminobutyric acid type A receptor(GABA_(A)R) is a γ-aminobutyric acid gated chloride ion channel. The agonist activity in vitro screening has relied on voltage clamp technique, which is expensive, high and low efficiency of operation, therefore our project synthesized a new fluorescent named C4, using γ-aminobutyric acid as agonist, to build a method for α1β2γ2 GABA;R agonists activity in vitro fluorescence screening. The research shows that the activity of γ-aminobutyric acid can be screened well and the EC_(50)value(29.44 ± 7.45 μM) also can be calculated from this in vitro fluorescence screening when using 100 μM C4. This EC_(50)value is very close comparing to that obtained by voltage clamp technique. Above all, this method achieves high throughput, rapid and convenient operation, and accurate screening requirements, it also provides a theoretical basis and technical support for other neural receptor agonist activity in vitro screening.

关 键 词：氨基丁酸A型受体 激动剂 C4 体外活性筛选 

分 类 号：TQ617.3[化学工程—精细化工] O657.3[理学—分析化学] TQ460.1[理学—化学]