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TACT908

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Pharmaceutical compound
TACT908
Clinical data
Other namesTACT-908; Compound 28-12; 2ZEDMA; [2-(Indolizin-1-yl)ethyl]dimethylamine; Indolizine-DMT
Drug classSerotonin receptor agonist;Serotonin5-HT1B receptoragonist; Non-hallucinogenicserotonin5-HT2A receptoragonist
Identifiers
  • 2-indolizin-1-yl-N,N-dimethylethanamine
PubChemCID
Chemical and physical data
FormulaC12H16N2
Molar mass188.274 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 aserotonin receptor agonist of theindolizinylethylamine family which is under development for the treatment ofcluster headaches.[1][2][3] It is apositional isomer of the famoustryptamineserotonergic psychedelicN,N-dimethyltryptamine (DMT) in which theindolering has been replaced with anindolizine ring.[1]

The drug acts as aserotonin5-HT1B and5-HT2A receptoragonist.[1][3] ItsEC50Tooltip half-maximal effective concentration at the serotonin 5-HT2A receptor is 52 nM (EmaxTooltip maximal efficacy ≈ 30% of that of serotonin) and itsEC50 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 screenedtargets, including the serotonin5-HT1A,5-HT2B, and5-HT3 receptors as well as themonoamine transporters (MATs).[1] Otherserotonin receptors besides the preceding, such as the serotonin5-HT2C receptor, were not assessed.[1] The drug was a weakmonoamine oxidase inhibitor (MAOI), specifically ofmonoamine oxidase A (MAO-A) (IC50Tooltip half-maximal inhibitory concentration = 7,252 nM).[1]

TACT908 is under development byTactogen.[1][2][3] It waspatented byMatthew Baggott of Tactogen in 2023.[1] As of January 2025, the drug is inpreclinical research for cluster headaches.[2][3]

The α-methyl andN-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 ofα,N-dimethyltryptamine (α,N-DMT orN-methyl-αMT).[1] 1ZP2MA was found to be apotentdopamine releasing agent, with anEC50 of 62 nM.[1]

See also

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References

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  1. ^abcdefghijklmWO patent 2023183613A2, Matthew J. Baggott, "Indolizine compounds for the treatment of mental disorders or inflammation", published 2023 September 28, assigned toTactogen 
  2. ^abcHaichin M (2024)."Psychedelics Drug Development Tracker".Psychedelic Alpha. Retrieved29 January 2025.
  3. ^abcde"Tactogen Inc – Pipeline".Tactogen Inc.Tactogen. 8 February 2021. Retrieved29 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.

External links

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5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Non-specific
AAADTooltip Aromatic L-amino acid decarboxylase
MAOTooltip Monoamine oxidase
Phenethylamines
(dopamine,epinephrine,
norepinephrine)
PAHTooltip Phenylalanine hydroxylase
THTooltip Tyrosine hydroxylase
DBHTooltip Dopamine beta-hydroxylase
PNMTTooltip Phenylethanolamine N-methyltransferase
COMTTooltip Catechol-O-methyl transferase
Tryptamines
(serotonin,melatonin)
TPHTooltip Tryptophan hydroxylase
AANATTooltip Serotonin N-acetyl transferase
ASMTTooltip Acetylserotonin O-methyltransferase
Histamine
HDCTooltip Histidine decarboxylase
HNMTTooltip Histamine N-methyltransferase
DAOTooltip Diamine oxidase


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