Photoswitchable TCB-2 for control of the 5-HT2A receptor and analysis of biased agonism

Alireza Jafar Esmaeili; Pantea Montazeri; Jasmine Cristina Gomez; Didier J. Dumervil; Faezeh Safar Nezhad; Rachel C. Steinhardt

doi:10.1039/D4CC03892D

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Photoswitchable TCB-2 for control of the 5-HT_2A receptor and analysis of biased agonism†

Alireza Jafar Esmaeili,‡^a Pantea Montazeri,‡^a Jasmine Cristina Gomez,^a Didier J. Dumervil,^a Faezeh Safar Nezhad^a and Rachel C. Steinhardt

*^a

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* Corresponding authors

^a Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA
E-mail: rcsteinh@syr.edu

Abstract

Therapies that target the serotonin 2A receptor (5-HT_2AR) are promising. However, probes are needed to better understand the role of 5-HT_2AR. Here, we design and synthesize a photoswitch and photoswitchable 5-HT_2AR ligand based on highly potent agonist TCB-2 and arylazopyrazole, which also boasts photoswitchable G protein vs. β-arrestin pathway bias.

This article is part of the themed collection: 2024 Emerging Investigators

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Article information

DOI: https://doi.org/10.1039/D4CC03892D
Article type: Communication
Submitted: 01 Ago 2024
Accepted: 24 Sep 2024
First published: 25 Sep 2024
This article is Open Access

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Chem. Commun., 2024, Advance Article

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Photoswitchable TCB-2 for control of the 5-HT_2A receptor and analysis of biased agonism

A. J. Esmaeili, P. Montazeri, J. C. Gomez, D. J. Dumervil, F. S. Nezhad and R. C. Steinhardt, Chem. Commun., 2024, Advance Article , DOI: 10.1039/D4CC03892D

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