Drug intelligence / Profile preview

bretisilocin

Development stage
Phase 2
Lead developer
AbbVie
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Bretisilocin (GM-2505) is a novel serotonergic psychedelic of the tryptamine family under development for the treatment of major depressive disorder. It is an analogue of dimethyltryptamine (DMT) and the 5-fluorinated derivative of methylethyltryptamine (MET). The drug acts as a potent serotonin 5-HT2A receptor and serotonin 5-HT2C receptor agonist, a serotonin 5-HT2B receptor antagonist or partial agonist, and a serotonin releasing agent. Additionally, it has been shown to act as a low potency reversible inhibitor of monoamine oxidase A (MAO-A) and as an antagonist at the serotonin transporter (SERT). Bretisilocin produces robust hallucinogenic effects with an intravenous duration of action between 60–90 minutes—intermediate between DMT and psilocybin—and is regarded by its developer as an improvement over DMT due to its more balanced pharmacological profile. As of early 2024, it is in phase II clinical trials for major depressive disorder[1][2][3][6].

Other names
5-fluoro-N-methyl-N-ethyltryptamine5F-MET5-fluoro-MET5-F-MET
02

Targets

SERT (Sodium-dependent serotonin transporter)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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