TACT908

Last updated

TACT908
TACT908.svg
Clinical data
Other namesTACT-908; Compound 28-12; 2ZEDMA; [2-(Indolizin-1-yl)ethyl]dimethylamine; Indolizine-DMT
Drug class Serotonin receptor agonist; Serotonin 5-HT1B receptor agonist; Non-hallucinogenic serotonin 5-HT2A receptor agonist
Identifiers
  • 2-indolizin-1-yl-N,N-dimethylethanamine
PubChem CID
Chemical and physical data
Formula C12H16N2
Molar mass 188.274 g·mol−1
3D model (JSmol)
  • CN(C)CCC1=C2C=CC=CN2C=C1
  • InChI=1S/C12H16N2/c1-13(2)9-6-11-7-10-14-8-4-3-5-12(11)14/h3-5,7-8,10H,6,9H2,1-2H3
  • Key:CBZZXMYTGARRHB-UHFFFAOYSA-N

TACT908, also known as [2-(indolizin-1-yl)ethyl]dimethylamine (2ZEDMA), is a serotonin receptor agonist which is under development for the treatment of cluster headaches. [1] [2] [3] It is an positional isomer of the famous tryptamine serotonergic psychedelic N,N-dimethyltryptamine (DMT) in which the indole ring has been replaced with an indolizine ring. [1]

The drug acts as a serotonin 5-HT1B and 5-HT2A receptor agonist. [1] [3] Its EC50 Tooltip half-maximal effective concentration at the serotonin 5-HT2A receptor is 52 nM (Emax Tooltip maximal efficacy ≈ 30% of that of serotonin) and its EC50 at the serotonin 5-HT1B receptor is 143 nM. [1] TACT908 is said to be a non-hallucinogenic serotonin 5-HT2A receptor agonist. [1] [3] 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). [1] Other serotonin receptors besides the preceding, such as the serotonin 5-HT2C receptor, were not assessed. [1] The drug was a weak monoamine oxidase inhibitor (MAOI), specifically of monoamine oxidase A (MAO-A) (IC50 Tooltip half-maximal inhibitory concentration = 7,252 nM). [1]

TACT908 is under development by Tactogen. [1] [2] [3] It was patented by Matthew Baggott and Tactogen in 2023. [1] As of January 2025, the drug is in preclinical research for cluster headaches. [2] [3]

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. [1] It is the indolizine analogue of α,N-dimethyltryptamine (α,N-DMT or N-methyl-αMT). [1] 1ZP2MA was found to be a potent dopamine releasing agent, with an EC50 of 62 nM. [1]

See also

References

  1. 1 2 3 4 5 6 7 8 9 10 11 12 13 WOpatent 2023183613A2, Matthew J. Baggott,"Indolizine compounds for the treatment of mental disorders or inflammation",published 2023 September 28, assigned to Tactogen
  2. 1 2 3 Haichin M (2024). "Psychedelics Drug Development Tracker". Psychedelic Alpha. Retrieved 29 January 2025.
  3. 1 2 3 4 5 "Tactogen Inc – Pipeline". Tactogen Inc. Tactogen. 8 February 2021. Retrieved 29 January 2025. OUR PIPELINE: [...] COMPOUND: TACT908. TARGETS: 5-HT1B, 5-HT2A ***. INDICATION: Cluster Headache. Prevalence: 0.24%. STATUS: Preclinical. [...] ***Partial agonist at 2A, non-hallucinogenic.



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