TACT908, also known as [2-(indolizin-1-yl)ethyl]dimethylamine (2ZEDMA), is a serotonin receptor agonist of the indolizinylethylamine family which is under development for the treatment of cluster headaches. It is a positional isomer of the tryptamine serotonergic psychedelic N,N-dimethyltryptamine (DMT) in which the indole ring has been replaced with an indolizine ring. The drug acts as a serotonin 5-HT1B and 5-HT2A receptor agonist. Its EC50Tooltip half-maximal effective concentration at the serotonin 5-HT2A receptor is 52 nM (EmaxTooltip maximal efficacy ≈ 30% of that of serotonin) and its EC50 at the serotonin 5-HT1B receptor is 143 nM. TACT908 is said to be a non-hallucinogenic serotonin 5-HT2A receptor agonist. It showed little or no activity at 45 other screened targets, including the serotonin 5-HT1A, 5-HT2B, and 5-HT3 receptors as well as the monoamine transporters (MATs). Other serotonin receptors besides the preceding, such as the serotonin 5-HT2C receptor, were not assessed. The drug was a weak monoamine oxidase inhibitor (MAOI), specifically of monoamine oxidase A (MAO-A) (IC50Tooltip half-maximal inhibitory concentration = 7,252 nM). TACT908 is under development by Tactogen. It was patented by Matthew Baggott of Tactogen in 2023. As of January 2025, the drug is in preclinical research for cluster headaches. The α-methyl and N-desmethyl analogue of TACT908, 1ZP2MA ([1-(indolizin-1-yl)propan-2-yl](methyl)amine or 1-(indolizin-1-yl)-N-methylpropan-2-amine), has also been characterized and described. It is the indolizine analogue of α,N-dimethyltryptamine (α,N-DMT or N-methyl-αMT). 1ZP2MA was found to be a potent dopamine releasing agent, with an EC50 of 62 nM.
See also Indolizinylethylamine Substituted tryptamine § Related compounds List of investigational hallucinogens and entactogens Non-hallucinogenic 5-HT2A receptor agonist N,N-Dimethylisotryptamine (isoDMT) 1Z2MAP1O C-DMT S-DMT TACT411 Rizatriptan TACT833
References
External links TACT908 (2ZEDMA) - Isomer Design



