Structural Pharmacology of Bufotenine Derivatives in Activating the 5-HT_1A Receptor for Therapeutic Potential in Depression and Anxiety.

ABSTRACT: The 5-HT_1A receptor is a critical target in the treatment of depression and anxiety. Bufotenine derivatives, such as 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), 5-hydroxy-N,N-dimethyltryptamine (5-OH-DMT), and 5-hydroxy-N,N,N-dimethyltryptamine-derived from traditional Chinese medicine-have shown antidepressant potential. However, the structural basis of their interaction with 5-HT_1A and their pharmacological profiles remain incompletely understood. This study investigated bufotenine derivatives acting on multiple serotonin receptors, highlighting 5-HT_1A as a key mediator of antidepressant effects while recognizing 5-HT_2A as primarily responsible for hallucinogenic outcomes, to identify candidate

SUBMITTER: Li SJ 

PROVIDER: S-EPMC12722636 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature