Photoswitchable TCB-2 for control of the 5-HT 2A receptor and analysis of biased agonism.

Autor: Esmaeili AJ; Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA. rcsteinh@syr.edu., Montazeri P; Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA. rcsteinh@syr.edu., Gomez JC; Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA. rcsteinh@syr.edu., Dumervil DJ; Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA. rcsteinh@syr.edu., Nezhad FS; Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA. rcsteinh@syr.edu., Steinhardt RC; Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA. rcsteinh@syr.edu.
Jazyk: angličtina
Zdroj: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2024 Oct 15; Vol. 60 (83), pp. 11956-11959. Date of Electronic Publication: 2024 Oct 15.
DOI: 10.1039/d4cc03892d
Abstrakt: Therapies that target the serotonin 2A receptor (5-HT 2A R) are promising. However, probes are needed to better understand the role of 5-HT 2A R. Here, we design and synthesize a photoswitch and photoswitchable 5-HT 2A R ligand based on highly potent agonist TCB-2 and arylazopyrazole, which also boasts photoswitchable G protein vs. β-arrestin pathway bias.
Databáze: MEDLINE