Skip to main content

4-AcO-MET

4-acetoxy-N-methyl-N-ethyltryptamine

6Node page

what any key link opens

psx:substance/4-aco-met/value/contraindication/dc2d84ff-16ca-48c8-9ca9-e499bfd7f7a6@1

valuereferenced by edges — no row of its own

derived from · upstream

feeds · downstream

none recorded

Closure of psx:substance/4-aco-met/value/contraindication/dc2d84ff-16ca-48c8-9ca9-e499bfd7f7a6@1: 1 upstream, 0 downstream.

psx:substance/4-aco-met/value/contraindication/dc2d84ff-16ca-48c8-9ca9-e499bfd7f7a6@1
└─ derived_from  proposal/contraindication/815bded6-ea56-4377-8cf5-ffed117dc6d4  contraindication · other

indented by distance from this node, not by parentage

1Provenance card

the boundary, as counts

Sources

1714 with DOI

2 strong · 12 moderate · 3 weak

Compilations

12026-04-26T12:49:03.299Z

pipeline-v5 · prompt hash not recorded — run predates 2026-09

Decisions

31last ruled 2026-06-04

0 awaiting a ruling

Issued documents

62026-10-19T20:29:51.174Z

notice · info card · emergency

Searches

192 with no results

queries and counts on the build

Claims checked

4836 supported

36 supported · 12 not

Correspondence

0received

consent field ships in Phase 4

Edges

180

derivations recorded for this entity

Complete over 17 sources, 1 compilation, and 31 decisions.Not here: the private journal (never).Working material — drafts, discards, unsupported claims — is listed below and readable on the working page.Cite: psychedex.org/substances/4-aco-met/archive

2Build

one panel per compilation run

generation run 2026-04-26

48 min completedmodel pipeline-v5plan not recordedrun/01526e13…

Selection

results seen43
selected by the model21
consumed as sources17

Verification

claims checked48
supported31
partially supported5
not supported0
inconclusive12
  • record
  • seen / partial
  • working

The model's own caveats

none raised on this run

Reproduce

inputs
17 source keys (listed under Sources)
plan
not recorded — template version, prompt hash and git SHA are written from 2026-09 onward
model
pipeline-v5
streams
none — agent transcripts are persisted from 2026-09 onward
19 searches — query, source, results, what was kept and why
19 searches for this run
#sourcequeryseenkeptrationale
1Web Search4-AcO-MET legal status scheduling controlled substance UK US Australia52—
2PubMed · absence4-AcO-MET 4-acetoxy-MET tryptamine psychedelic0——
3PubMedPMID 3666987511—
4PubMedpsilocin analogs acetoxy tryptamine receptor binding pharmacology11Closest 4-acetoxy tryptamine metabolic pathway study to 4-AcO-MET
5WebFetch—1——
6PubMedPMID 2626528511—
7OpenAlex4-AcO-MET 4-acetoxy-MET tryptamine psychedelic105Direct pharmacology, crystal structure, and safety case reports
8WebFetch—1——
9PubChem4-AcO-MET11Primary chemical identity source
10PubMedtramadol serotonin syndrome seizure drug interaction tryptamine11—
11WebSearch4-HO-MET metocin pharmacology synthesis Shulgin TiHKAL first synthesis 1997102—
12WebFetch—11—
13PubMed4-AcO-DMT psilacetin metabolite identification urinary biomarker forensic11—
14PubMedRepke tryptamine synthesis hydroxytryptamine 4-hydroxy pharmacology11—
15WebSearch4-AcO-MET Switzerland Verzeichnis E Germany NpSG scheduling controlled51—
16PubMedIdentification New Psychoactive Tryptamines 4-OH-MET11—
17PubMedpsychedelic 5-HT2A receptor agonist tolerance rapid tachyphylaxis11—
18PubMedin silico toxicity tryptamine psilocin psilocybin O-acetylpsilocin computational11—
19ClinicalTrials.gov · absence4-AcO-MET tryptamine psychedelic00—
48 claims by section — every cited sentence, checked against its source
safety16 · 9 ok
  • Jurowski et al. performed in silico toxicity assessment of the closest structural analog, 4-AcO-DMT, predicting an oral LD₅₀ in the 100–500 mg/kg range (Cramer Class III, moderate-to-high acute toxicity)supported

    In silico toxicology of 6 tryptamines including 4-AcO-DMT. Predicted oral LD50 100-500 mg/kg. Cramer Class III. s00204-026-04365-4

  • Cardiovascular and gastrointestinal systems were identified as primary predicted target organs (≥90% predicted probability). 4-AcO-DMT was predicted to be non-mutagenic and non-endocrine-activepartially supported

    Cardiovascular and GI primary targets. Non-mutagenic predicted. s00204-026-04365-4

  • Claim in safety — inconclusiveinconclusiveworking →

  • McIntyre et al. reported a fatality in which 4-HO-MET was detected by GC-MS in postmortem specimenssupported

    4-HO-MET (active metabolite of 4-AcO-MET) also detected by GC-MS, not quantified. bkv089

  • Malaca et al. reviewed tryptamine toxicology broadly, finding that morbidity from novel psychoactive tryptamines is underestimated and that tryptamines are typically absent from standard toxicology screening panelspartially supported

    Review of tryptamine toxicology. 22 new analytical methods 2015-2020. Morbidity considerable and underestimated. ijms21239279

  • Kopra et al. analyzed psychedelic-related fatalities in England, Wales, and Northern Ireland (1997–2022), finding that deaths directly attributable to classical serotonergic psychedelics are rare relative to other drug classes.supported

    Systematic characterization of psychedelic-related deaths 1997-2022. Fatalities associated with psychedelics appear rare. j.pnpbp.2024.111177

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • De la Fuente Revenga et al. demonstrated in mice that repeated psychedelic administration produces progressive decreases in head twitch response (a behavioral proxy for psychedelic effect), with single-dose tolerance observable within 24 hourssupported

    Repeated psychedelic administration causes progressive HTR decrease. Single-dose tolerance after 24h. acschemneuro.2c00170

  • Cross-tolerance extends between structurally distinct psychedelics (DOI and LSD were tested), indicating a shared mechanism of 5-HT₂A receptor downregulation in frontal cortex independent of β-arrestin-2.partially supported

    Cross-tolerance between DOI and LSD. 5-HT2AR downregulation in frontal cortex. acschemneuro.2c00170

  • Claim in safety — inconclusiveinconclusiveworking →

  • {{Warning}}Tramadol: Tramadol inhibits the serotonin transporter (SERT) and has been linked by the FDA to serotonin toxicity risksupported

    Tramadol inhibits human SERT in vitro; combined with serotonergic drugs, can precipitate serotonin syndrome. FDA Drug Safety Communication 2016. s00204-018-2244-6

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Contraindication data for 4-AcO-MET are inferred from psilocybin class-level pharmacologysupported

    Practical guidance for psilocybin therapy including pharmacology, pharmacokinetics, dosing, contraindications, adverse events, drug interactions. fpsyt.2022.1040217

receptor-pharmacology8 · 6 ok
  • The 4-substituted compounds demonstrated high selectivity for the 5-HT₂A receptorsupported

    4-substituted compounds show high selectivity for 5-HT2AR. jpet.122.001454

  • The 4-acetoxy and 4-propionoxy analogs displayed somewhat weaker binding affinities than the corresponding 4-hydroxy compounds but maintained similar target profiles across serotonin receptor subtypessupported

    4-acetoxy analogues show somewhat weaker binding affinities but similar target profiles to 4-hydroxy compounds. acsptsci.2c00222

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

  • The foundational selectivity data for 4-hydroxylated tryptamines derives from McKenna et al., who established that this class displays 25–380-fold selectivity for 5-HT₂A over 5-HT₁A in radioligand binding assayssupported

    4-hydroxylated derivatives show 25-380-fold selectivity for 5-HT2A vs 5-HT1A. pmid:2139186

  • Within this class, N,N-dialkyl chain length modulates affinity: short chains (dimethyl, methyl-ethyl) retain high affinity, while bulky substituents (diisopropyl and larger) substantially reduce binding at both 5-HT₂A and 5-HT₁A.supported

    N,N-dialkyl size secondary determinant; groups larger than diisopropyl markedly reduce affinity. pmid:2139186

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

  • {{Info}}Quantitative Ki and EC₅₀ values for 4-AcO-MET at individual receptor targets are known to exist in the Kozell et al. and Glatfelter et al. publications but could not be retrieved during research due to access restrictionssupported

    Includes 4-AcO-MET in binding panel. jpet.122.001454

  • {{Info}}Quantitative Ki and EC₅₀ values for 4-AcO-MET at individual receptor targets are known to exist in the Kozell et al. and Glatfelter et al. publications but could not be retrieved during research due to access restrictionssupported

    Includes 4-AcO-MET binding data. acsptsci.2c00222

pharmacology6 · 6 ok
  • Following oral administration, the acetate ester is expected to undergo rapid hydrolysis by serum esterases to yield the active metabolite 4-HO-METsupported

    Primary: hydrolysis to psilocin. dta.3255

  • This prodrug-to-active-metabolite conversion parallels the established pathway of 4-AcO-DMT to psilocin, for which Zhai et al. demonstrated that ester hydrolysis is the predominant phase I metabolic transformation in pooled human liver microsomessupported

    4-AcO-DMT metabolism in pooled human liver microsomes. Primary: hydrolysis to psilocin. dta.3255

  • McKenna et al. demonstrated in radioligand competition assays that 4-hydroxylated indolealkylamines as a class display 25–380-fold selectivity for the 5-HT₂A receptor over 5-HT₁Asupported

    Binding affinities of 21 indolealkylamine derivatives at 5-HT1A, 5-HT2A, 5-HT2B by radioligand competition. 4-hydroxylated derivatives show 25-380-fold selectivity for 5-HT2A vs 5-HT1A. pmid:2139186

  • The N-methyl-N-ethyl substitution pattern falls within the range associated with preserved high 5-HT₂A affinity; N,N-dialkyl groups larger than N,N-diisopropyl markedly reduce binding at both 5-HT₂A and 5-HT₁A sites.supported

    N,N-dialkyl size secondary determinant; groups larger than diisopropyl markedly reduce affinity. pmid:2139186

  • Zhai et al. identified additional phase I pathways for 4-AcO-DMT including hydroxylation, N-demethylation, and oxidation, with phase II conjugation (glucuronidation) also observedsupported

    Phase II: glucuronidation, sulfation. N-demethylation, hydroxylation. dta.3255

  • Malaca et al. confirmed analogous metabolic transformation for 4-AcO-DiPT in human hepatocyte preparations — hydrolysis to the 4-hydroxy metabolite followed by N-dealkylation, oxidation, glucuronidation, and sulfation. 4-AcO-MET is expected to follow an analogous biotransformation sequence, but this remains unverified.supported

    4-AcO-DiPT metabolism in human hepatocytes. Primary metabolite via ester hydrolysis is 4-OH-DiPT. Phase II: glucuronidation and sulfation. N-oxidation and N-dealkylation also occur. metabo12080705

summary6 · 5 ok
  • Its solid-state crystal structure was confirmed by X-ray diffraction in 2021.supported

    Solid-state structures of three psilacetin derivatives including 4-AcO-MET (4-acetoxy-N-ethyl-N-methyl-tryptammonium) hydrofumarate salt. s2056989021000116

  • The 4-hydroxylated tryptamine class displays 25–380-fold selectivity for 5-HT₂A over 5-HT₁A, and receptor binding panels confirm high 5-HT₂A selectivity for 4-substituted tryptamines including 4-AcO-MET specificallypartially supported

    4-hydroxylated derivatives show 25-380-fold selectivity for 5-HT2A vs 5-HT1A. pmid:2139186

  • The 4-hydroxylated tryptamine class displays 25–380-fold selectivity for 5-HT₂A over 5-HT₁A, and receptor binding panels confirm high 5-HT₂A selectivity for 4-substituted tryptamines including 4-AcO-MET specificallysupported

    4-substituted compounds show high selectivity for 5-HT2AR. Includes 4-AcO-MET in binding panel. jpet.122.001454

  • In silico modelling of the structural analog 4-AcO-DMT predicts an oral LD₅₀ in the 100–500 mg/kg range (Cramer Class III), but this has not been experimentally validatedsupported

    In silico toxicology of 6 tryptamines including 4-AcO-DMT. Predicted oral LD50 100-500 mg/kg. Cramer Class III. s00204-026-04365-4

  • Tolerance develops rapidly via 5-HT₂A receptor downregulation, with single-dose tolerance observable within 24 hours and full reset within approximately 7 dayspartially supported

    Single-dose tolerance after 24h. 5-HT2AR downregulation in frontal cortex. acschemneuro.2c00170

  • Claim in summary — inconclusiveinconclusiveworking →

comparative-pharmacology3 · 1 ok
  • Glatfelter et al. tested this matrix and established that 4-acetoxy compounds display somewhat weaker binding affinities than the corresponding 4-hydroxy analogs but maintain similar receptor target profiles across serotonin receptor subtypessupported

    4-acetoxy analogues show somewhat weaker binding affinities but similar target profiles to 4-hydroxy compounds. acsptsci.2c00222

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

chemistry2 · 2 ok
  • These identifiers were confirmed via PubChem CID 71308138 and are consistent with the X-ray crystal structure reported by Pham et al.supported

    Solid-state structures of three psilacetin derivatives including 4-AcO-MET (4-acetoxy-N-ethyl-N-methyl-tryptammonium) hydrofumarate salt. s2056989021000116

  • The X-ray crystal structure of 4-AcO-MET hydrofumarate (C₁₅H₂₁N₂O₂⁺·C₄H₃O₄⁻) reveals a protonated tryptammonium cation paired with a fumarate anion, consolidated by N–H···O and O–H···O hydrogen bondssupported

    4-AcO-MET (4-acetoxy-N-ethyl-N-methyl-tryptammonium) hydrofumarate salt. Crystal structure consolidation via N-H...O and O-H...O hydrogen bonds. s2056989021000116

clinical-evidence2 · 2 ok
  • McIntyre et al. reported a fatality in which 4-HO-MET (the active metabolite of 4-AcO-MET) was detected by GC-MS in postmortem toxicologysupported

    4-HO-MET (active metabolite of 4-AcO-MET) also detected by GC-MS, not quantified. bkv089

  • Co-medications included venlafaxine, olanzapine, lorazepam, and hydroxyzine at therapeutic concentrationssupported

    Co-medications: venlafaxine, olanzapine, lorazepam, hydroxyzine at therapeutic levels. bkv089

history2 · 2 ok
  • The solid-state X-ray crystal structure of 4-AcO-MET hydrofumarate was determined by Pham et al. in 2021, confirming the molecular geometry of the protonated tryptammonium cation paired with a fumarate counterion (C₁₅H₂₁N₂O₂⁺·C₄H₃O₄⁻)supported

    Solid-state structures of three psilacetin derivatives including 4-AcO-MET (4-acetoxy-N-ethyl-N-methyl-tryptammonium) hydrofumarate salt. Crystal structure consolidation via N-H...O and O-H...O hydrogen bonds. s2056989021000116

  • In 2021, Ding et al. identified 4-OH-MET (the active metabolite) in seized drug material in China, using GC-QTOF-MS and UPLC-LTQ-Orbitrap MS with NMR confirmationsupported

    4-OH-MET identified in white powder from actual drug case by GC-QTOF-MS, UPLC-LTQ-Orbitrap MS and 1H-NMR. j.issn.1004-5619.2021.310305

pharmacokinetic-detail2 · 2 ok
  • 4-AcO-DMT (N,N-dimethyl analog): Zhai et al. characterized in vitro phase I metabolism in pooled human liver microsomes using UHPLC-Q-Orbitrap MS. Ester hydrolysis to psilocin (4-HO-DMT) was the most abundant metabolic pathway. Additional phase I metabolites arose from hydroxylation, N-demethylation, and oxidation. Phase II metabolism included glucuronide conjugation.supported

    4-AcO-DMT metabolism in pooled human liver microsomes. 15 metabolites. Primary: hydrolysis to psilocin. Phase II: glucuronidation, sulfation. N-demethylation, hydroxylation. dta.3255

  • 4-AcO-DiPT (N,N-diisopropyl analog): Malaca et al. profiled metabolism in human hepatocyte preparations using LC-HRMS/MS. The predominant pathway was ester hydrolysis to 4-HO-DiPT, followed by N-dealkylation, oxidation, glucuronidation, and sulfation.supported

    4-AcO-DiPT metabolism in human hepatocytes. Primary metabolite via ester hydrolysis is 4-OH-DiPT. Phase II: glucuronidation and sulfation. N-oxidation and N-dealkylation also occur. metabo12080705

neuroscience1 · 1 ok
  • How do the differential non-serotonergic binding profiles across the N,N-dialkyl series translate to differences in neural activation and subjective experience?supported

    Receptor binding profiles for tryptamine psychedelics with 4-position (hydroxy, acetoxy, propionoxy) and N,N-dialkyl substitutions. Includes 4-AcO-MET binding data. acsptsci.2c00222

3Sources

17 consumed · sorted by year · feeds = sections resting on it

Sources
yearsourcetierstatusfeeds
2026In-silico toxicity study of tryptamine, psilocin, psilocybin, N,N-dimethyltryptamine, 5'-methoxy-N,N-dimethyltryptamine and O-acetylpsilocinJurowski K, Kobylarz D, Noga M · Archives of Toxicologydoi:10.1007/s00204-026-04365-4moderateconsumed2 sections
2025Psychedelic-related deaths in England, Wales and Northern Ireland (1997-2022)Kopra EI, Penttinen J, Rucker JJ, Copeland CS · Progress in Neuro-Psychopharmacology & Biological Psychiatrydoi:10.1016/j.pnpbp.2024.111177moderateconsumed1 section
20234-AcO-MET (HandWiki)HandWiki contributorsurl:ec53d42944eb1ad7weakconsumedcited only
2023Pharmacologic Activity of Substituted Tryptamines at 5-HT2A, 5-HT2C, 5-HT1A Receptors and SERTKozell LB, Eshleman AJ, Swanson TL, Bloom SH, Wolfrum KM, et al. · Journal of Pharmacology and Experimental Therapeuticsdoi:10.1124/jpet.122.001454moderateconsumed2 sections
2023Receptor Binding Profiles for Tryptamine Psychedelics and Effects of 4-Propionoxy-N,N-dimethyltryptamine in MiceGlatfelter GC, Naeem M, Pham DNK, Golen JA, Chadeayne AR, Manke DR, Baumann MH · ACS Pharmacology & Translational Sciencedoi:10.1021/acsptsci.2c00222strongconsumed3 sections
2022Adverse effects of psychedelics: From anecdotes and misinformation to systematic scienceSchlag AK, Aday J, Salam I, Neill JC, Nutt DJ · Journal of Psychopharmacologydoi:10.1177/02698811211069100moderateconsumed2 sections
2022Human Hepatocyte 4-Acetoxy-N,N-Diisopropyltryptamine Metabolite Profiling by LC-HRMS/MSMalaca S, Huestis MA, Lattanzio L, Marsella LT, Tagliabracci A, Carlier J, Busardo FP · Metabolitesdoi:10.3390/metabo12080705moderateconsumed2 sections
2022Tentative identification of in vitro metabolites of O-acetylpsilocin (psilacetin, 4-AcO-DMT) by UHPLC-Q-Orbitrap MSZhai W, Li L, Zhao J, Xiang P, Liu M, Shi Y, Dang Y · Drug Testing and Analysisdoi:10.1002/dta.3255strongconsumed2 sections
2022Therapeutic use of psilocybin: Practical considerations for dosing and administrationMacCallum CA, Lo LA, Pistawka CA, Deol JK · Frontiers in Psychiatrydoi:10.3389/fpsyt.2022.1040217moderateconsumed2 sections
2022Tolerance and Cross-Tolerance among Psychedelic and Nonpsychedelic 5-HT2A Receptor Agonists in Micede la Fuente Revenga M, Jaster AM, McGinn J, Silva G, Saha S, Gonzalez-Maeso J · ACS Chemical Neurosciencedoi:10.1021/acschemneuro.2c00170moderateconsumed2 sections
2021Identification of New Psychoactive Tryptamines 4-OH-MET and 4-AcO-DMT Using High Resolution Mass Spectrometry and Nuclear Magnetic Resonance SpectroscopyDing KR, Ni CF, He SY, Wang KD, Deng QY, Liang C · Fa Yi Xue Za Zhidoi:10.12116/j.issn.1004-5619.2021.310305moderateconsumed1 section
2021Psilacetin derivatives: fumarate salts of the methyl-ethyl, methyl-allyl and diallyl variants of the psilocin prodrugPham DNK, Chadeayne AR, Golen JA, Manke DR · Acta Crystallographica Section E Crystallographic Communicationsdoi:10.1107/s2056989021000116moderateconsumedcited only
2020Toxicology and Analysis of Psychoactive Tryptamines.Malaca S, Lo Faro AF, Tamborra A, Pichini S, Busardò FP, Huestis MA · International journal of molecular sciencesdoi:10.3390/ijms21239279moderateconsumed1 section
2018Opioid analgesic drugs and serotonin toxicity (syndrome): mechanisms, animal models, and links to clinical effectsBaldo BA · Archives of Toxicologydoi:10.1007/s00204-018-2244-6moderateconsumed1 section
2015A Fatality Related to Two Novel Hallucinogenic Compounds: 4-Methoxyphencyclidine and 4-Hydroxy-N-methyl-N-ethyltryptamineMcIntyre IM, Trochta A, Gary RD, Storey A, Corneal J, Schaber B · Journal of Analytical Toxicologydoi:10.1093/jat/bkv089weakconsumed2 sections
1997TiHKAL #21: 4-HO-MET (Erowid online reproduction)Shulgin A, Shulgin Aurl:5709ad0cbf25573cweakconsumedcited only
1990Differential interactions of indolealkylamines with 5-hydroxytryptamine receptor subtypesMcKenna DJ, Repke DB, Lo L, Peroutka SJ · Neuropharmacologypmid:2139186moderateconsumed4 sections
—Searched ClinicalTrials.gov for "4-AcO-MET tryptamine psychedelic" — no resultsabsenceno results—
—Searched PubMed for "4-AcO-MET 4-acetoxy-MET tryptamine psychedelic" — no resultsabsenceno results—

4Docket

one filing per activity — decisions, correspondence, reports

  1. 0012026-04-26revisionRevision 1

    Initial LLM generation (v5 pipeline, wiki)

    psx:substance/4-aco-met/version/1
  2. 0022026-06-04proposal29 value proposals approved together

    one review action inferred from a shared reviewer and instant — the graph records one activity per proposal

    29 items in this filing

    • dose_tier · light
    • dose_tier · common
    • dose_tier · strong
    • dose_tier · heavy
    • timeline · oral · onset
    • timeline · oral · come_up
    • timeline · oral · peak
    • timeline · oral · plateau
    • timeline · oral · resolution
    • timeline · oral · afterglow
    • toxicity
    • dependence · full
    • withdrawal
    • tolerance
    • dosage · oral
    • duration · oral · onset
    • duration · oral · come_up
    • duration · oral · peak
    • duration · oral · offset
    • duration · oral · total
    • duration · oral · aftereffects
    • contraindication · psychiatric
    • contraindication · psychiatric
    • contraindication · other
    • contraindication · other
    • contraindication · other
    • contraindication · pregnancy_breastfeeding
    • contraindication · cardiovascular
    psx:substance/4-aco-met/proposal/dose_tier/24b139f5-6690-49c9-8450-144f80211d26
  3. 0032026-06-04publicationPublication — backfill

5Issued documents

what the notice, info card and emergency page said, by hash

Issued documents
documentcontent hashissuedfrom versionsuperseded
emergencyc15c760aabf6f0fcf5b6fc6b…2026-10-19 20:29Revision 1current
info_card87ba028455cb1b7511af14b8…2026-10-19 20:29Revision 1current
noticef069a9dea47b308467344618…2026-10-19 20:29Revision 1current
emergency3f0909c25c714d225b4bb3e3…2026-09-04 04:27Revision 1superseded2026-10-19
info_cardb3e9c8b3703695efd8168592…2026-09-04 04:27Revision 1superseded2026-10-19
notice64878b43a1d2932a5305f55b…2026-09-04 04:27Revision 1superseded2026-10-19