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

页码：1231 / 1237

页数：7

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