Drug intelligence / Profile preview

TACT908

Development stage
Preclinical
Lead developer
Tactogen
Modality
Small Molecules
01

Overview

TACT908 is a non-hallucinogenic serotonin receptor agonist under development for the treatment of cluster headaches. Chemically known as [2-(indolizin-1-yl)ethyl]dimethylamine (2ZEDMA), it is a positional isomer of N,N-dimethyltryptamine (DMT), with the indole ring replaced by an indolizine ring. TACT908 acts primarily as an agonist at the serotonin 5-HT2A and 5-HT1B receptors, with EC50 values of 52 nM and 143 nM respectively. Its efficacy at the 5-HT2A receptor reaches about 30% of that of serotonin itself. The compound shows little or no activity at other tested targets, including other serotonin receptors such as 5-HT1A, 5-HT2B, and monoamine transporters. It also exhibits weak inhibition of monoamine oxidase A (IC50 = 7,252 nM). As of January 2025, TACT908 remains in preclinical research for cluster headache therapy[1][5].

02

Targets

HTR1B (5-Hydroxytryptamine Receptor 1B)HTR2A (Serotonin receptor 5-HT2A)MAOA (Monoamine oxidase A)

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