Chemistry:5-Fluoro-AET

From HandWiki

5-Fluoro-AET, also known as 5-fluoro-α-ethyltryptamine or by the code name PAL-545, is a substituted tryptamine derivative which acts as a serotonin–dopamine releasing agent (SDRA) and as an agonist of the serotonin 5-HT2A receptor.[1]

Pharmacology

Pharmacodynamics

Its EC50 values for monoamine release are 36.6 nM for serotonin, 5,334 nM for norepinephrine, and 150 nM for dopamine in rat brain synaptosomes.[1] Its EC50 at the serotonin 5-HT2A receptor is 246 nM and its Emax at the receptor is 87%.[1]

Several close analogues of 5-fluoro-αET, including 5-fluoro-αMT and 5-chloro-αMT, are known to be potent monoamine oxidase inhibitors (MAOIs), specifically of monoamine oxidase A (MAO-A).[2] However, α-ethyltryptamine (αET) is a very weak MAOI.[3][4] 5-Fluoro-αET has also more recently been assessed, and in contrast to αET, but similarly to drugs like 5-fluoro-αET, was found to be a potent MAOI, with an IC50 of 2,480 nM.[5] Potent monoamine oxidase inhibition by monoamine releasing agents (MRAs) has been associated with dangerous and sometimes fatal toxicity in humans.[2]

Chemistry

Analogues

Analogues of 5-fluoro-AET include α-ethyltryptamine (AET), 5-fluorotryptamine, 4-methyl-AET, 5-chloro-AET, 5-chloro-AMT, 5-fluoro-AMT, 5-fluoro-DMT, bretisilocin (5-fluoro-MET), 5-MeO-AET, 6-fluoro-AMT, 7-chloro-AMT, 7-methyl-DMT, and 7-methyl-AET, among others.

Society and culture

Canada

5-Fluoro-AET is not an explicitly nor implicitly controlled substance in Canada as of 2025.[6]

United States

5-Fluoro-AET is not an explicitly controlled substance in the United States.[7] However, it could be considered a controlled substance under the Federal Analogue Act if intended for human consumption.

See also

  • Substituted α-alkyltryptamine

References

  1. ↑ 1.0 1.1 1.2 "Alpha-ethyltryptamines as dual dopamine-serotonin releasers". Bioorganic & Medicinal Chemistry Letters 24 (19): 4754–4758. October 2014. doi:10.1016/j.bmcl.2014.07.062. PMID 25193229. 
  2. ↑ 2.0 2.1 "Amphetamine Derivatives as Monoamine Oxidase Inhibitors". Front Pharmacol 10. 2019. doi:10.3389/fphar.2019.01590. PMID 32038257. "Several close analogues of 5-chloro-αET, such as 5-chloro-αMT and 5-fluoro-αMT, are known to be potent monoamine oxidase inhibitors (MAOIs).". 
  3. ↑ "α-Ethyltryptamine: A Ratiocinatory Review of a Forgotten Antidepressant". ACS Pharmacology & Translational Science 6 (12): 1780–1789. December 2023. doi:10.1021/acsptsci.3c00139. PMID 38093842. 
  4. ↑ "Selective inhibition of monoamine oxidase in monoaminergic neurons in the rat brain". Naunyn-Schmiedeberg's Archives of Pharmacology 324 (2): 79–87. September 1983. doi:10.1007/BF00497011. PMID 6646243. 
  5. ↑ Matthew Baggott, "Advantageous tryptamine compositions for mental disorders or enhancement", WO patent 2022061242, published 2023 March 24, assigned to Tactogen
  6. ↑ "Controlled Drugs and Substances Act". 5 December 2025. https://laws-lois.justice.gc.ca/eng/acts/c-38.8/FullText.html. 
  7. ↑ Orange Book: List of Controlled Substances and Regulated Chemicals (January 2026), United States: U.S. Department of Justice: Drug Enforcement Administration (DEA): Diversion Control Division, January 2026, https://www.deadiversion.usdoj.gov/schedules/orangebook/orangebook.pdf 



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