Vern Lewis, Emma M Bonniwell, Janelle K Lanham, Abdi Ghaffari, Hooshmand Sheshbaradaran, Andrew B Cao, Maggie M Calkins, Mario Alberto Bautista-Carro, Emily Arsenault, Andre Telfer, Fatimeh-Frouh Taghavi-Abkuh, Nicholas J Malcolm, Fatema El Sayegh, Alfonso Abizaid, Yasmin Schmid, Kathleen Morton, Adam L Halberstadt, Argel Aguilar-Valles, John D McCorvy
Hallucinations limit widespread therapeutic use of psychedelics as rapidly acting antidepressants. Here we profiled the non-hallucinogenic lysergic acid diethylamide (LSD) analog 2-bromo-LSD (2-Br-LSD) at more than 33 aminergic G protein-coupled receptors (GPCRs). 2-Br-LSD shows partial agonism at several aminergic GPCRs, including 5-HT2A , and does not induce the head-twitch response (HTR) in mice, supporting its classification as a non-hallucinogenic 5-HT2A partial agonist. Unlike LSD, 2-Br-LSD lacks 5-HT2B agonism, an effect linked to cardiac valvulopathy...
March 6, 2023: Cell Reports