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 Aug 2024
Accepted: 24 Sep 2024
First published: 25 Sep 2024
This article is Open Access

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Chem. Commun., 2024,60, 11956-11959

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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, 60, 11956 DOI: 10.1039/D4CC03892D

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