School of Science, Harbin Institute of Technology (Shenzhen), Shenzhen 518055, China.
Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003, United States.
ACS Chem Neurosci. 2020 May 6;11(9):1231-1237. doi: 10.1021/acschemneuro.9b00521. Epub 2020 Apr 23.
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 and configurations using light of different wavelengths. The dark-adapted isomer was found to be significantly less active than the isomer, formed upon irradiation.
人类血清素转运蛋白（hSERT）通过将神经递质重新摄取到突触前神经元中来终止血清素能信号传递，是许多抗抑郁药物的靶标。我们在这里描述了一种光可开关的 hSERT 抑制剂的开发，称为偶氮-依地普仑，它可以使用不同波长的光在 和 两种构象之间可逆切换。发现暗适应的 异构体的活性明显低于照射后形成的 异构体。
