Azologization of serotonin 5-HT₃ receptor antagonists

• Karin Rustler,
• Galyna Maleeva,
• Piotr Bregestovski and
• Burkhard König

Beilstein J. Org. Chem. 2019, 15, 780–788, doi:10.3762/bjoc.15.74

• Medical University, Kazan, Russia Institute of Neurosciences, Kazan State Medical University, Kazan, Russia 10.3762/bjoc.15.74 Abstract The serotonin 5-hydroxytryptamine 3 receptor (5-HT3R) plays a unique role within the seven classes of the serotonin receptor family, as it represents the only ionotropic

• detailed receptor examination. In the presented work, we summarize the synthesis, photochromic properties and in vitro characterization of azobenzene-based photochromic derivatives of published 5-HT3R antagonists. Despite reported proof of principle of direct azologization, only one of the investigated

• derivatives showed antagonistic activity lacking isomer specificity. Keywords: azobenzene; 5-HT3R; ion currents; photopharmacology; serotonin; Introduction 5-Hydroxytryptamine (5-HT), commonly known as serotonin [1][2] or enteramine [3][4], is a monoamine neurotransmitter and hormone which is produced in