A Photoswitchable Inhibitor of the Human Serotonin Transporter

被引：15
|
作者：
Cheng, Bichu [2 ,3 ]
Morstein, Johannes [2 ]
Ladefoged, Lucy Kate [4 ]
Maesen, Jannick Bang [1 ]
Schiott, Birgit [4 ]
Sinning, Steffen [1 ]
Trauner, Dirk [2 ]
机构：
[1] Aarhus Univ, Dept Forens Med, DK-8200 Aarhus N, Denmark
[2] NYU, Dept Chem, New York, NY 10003 USA
[3] Harbin Inst Technol Shenzhen, Sch Sci, Shenzhen 518055, Peoples R China
[4] Aarhus Univ, Dept Chem, DK-8000 Aarhus C, Denmark
来源：
ACS CHEMICAL NEUROSCIENCE | 2020年 / 11卷 / 09期
基金：
美国国家卫生研究院;
关键词：
Photopharmacology; serotonin; transporter; photochromic ligand; neurotransmitter; LIGHT-INDUCED CONTROL; OPTICAL CONTROL; PHOTOCHROMIC AGONIST; BINDING-SITE; PROTEIN; MECHANISM; DISCOVERY;
D O I：
10.1021/acschemneuro.9b00521
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The human serotonin transporter (hSERT) terminates serotonergic signaling through reuptake of neurotransmitter into presynaptic neurons and is a target for many antidepressant drugs. We describe here the development of a photoswitchable hSERT inhibitor, termed azo-escitalopram, that can be reversibly switched between trans and cis configurations using light of different wavelengths. The dark-adapted trans isomer was found to be significantly less active than the cis isomer, formed upon irradiation.
引用
收藏
页码：1231 / 1237
页数：7
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