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

Autor: Esmaeili, Alireza Jafar, Montazeri, Pantea, Gomez, Jasmine Cristina, Dumervil, Didier J., Nezhad, Faezeh Safar, Steinhardt, Rachel C.
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Zdroj: Chemical Communications; 10/25/2024, Vol. 60 Issue 83, p11956-11959, 4p
Abstrakt: Therapies that target the serotonin 2A receptor (5-HT2AR) are promising. However, probes are needed to better understand the role of 5-HT2AR. Here, we design and synthesize a photoswitch and photoswitchable 5-HT2AR ligand based on highly potent agonist TCB-2 and arylazopyrazole, which also boasts photoswitchable G protein vs. β-arrestin pathway bias. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index