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psx:substance/tma-2/proposal/tolerance/6e1efa24-b4ca-4e4e-ad3b-dd53b59f8890

proposal2026-04-26recordapproved

derived from · upstream

none recorded

feeds · downstream

Closure of psx:substance/tma-2/proposal/tolerance/6e1efa24-b4ca-4e4e-ad3b-dd53b59f8890: 0 upstream, 1 downstream.

psx:substance/tma-2/proposal/tolerance/6e1efa24-b4ca-4e4e-ad3b-dd53b59f8890
└─ derived_from  value/tolerance@1

indented by distance from this node, not by parentage

1Provenance card

the boundary, as counts

Sources

1810 with DOI

0 strong · 14 moderate · 4 weak

Compilations

12026-04-26T20:56:07.989Z

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

Decisions

31last ruled 2026-06-04

0 awaiting a ruling

Issued documents

52026-10-19T20:34:20.975Z

notice · info card · emergency

Searches

151 with no results

queries and counts on the build

Claims checked

4728 supported

28 supported · 19 not

Correspondence

0received

consent field ships in Phase 4

Edges

173

derivations recorded for this entity

Complete over 18 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/tma-2/archive

2Build

one panel per compilation run

generation run 2026-04-26

55 min completedmodel pipeline-v5plan not recordedrun/b13707b3…

Selection

results seen47
selected by the model29
consumed as sources18

Verification

claims checked47
supported27
partially supported1
not supported2
inconclusive17
  • record
  • seen / partial
  • working

The model's own caveats

none raised on this run

Reproduce

inputs
18 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
15 searches — query, source, results, what was kept and why
15 searches for this run
#sourcequeryseenkeptrationale
1PubMedTMA-2 2,4,5-trimethoxyamphetamine pharmacology76All directly relevant to TMA-2 pharmacology, metabolism, and behavioral effects
2PubChemTMA-211Verified chemical identity data for TMA-2
3PubMedTMA-2 trimethoxyamphetamine head twitch response hallucinogen potency20Duplicates of previously found articles
4OpenAlexTMA-2 trimethoxyamphetamine psychedelic103Relevant for pharmacology context, behavioral comparisons, and forensic detection
5ClinicalTrials.gov · absenceTMA-2 trimethoxyamphetamine00No trials found
6PsychonautWikiTMA-2 dose duration history pharmacology10Confirmed existing dose/duration data, consistent with Shulgin PIHKAL
7PubChemTMA-2 CID 3101411Verified chemical identity data for TMA-2
8PubMedTMA drug discrimination DOM rat behavioral11Historical drug discrimination data for TMA series
9Web - European Monitoring CentreEMCDDA risk assessment TMA-2 200321Official EU drug risk assessment for TMA-2
10PubMed2,5-Dimethoxyamphetamine CYP2D6 metabolism TMA-222Key sources on TMA-2 metabolism and forensic detection
11Web - DEA, EMCDDA, Canada CDSATMA-2 legal status scheduling53Primary legal sources for TMA-2 scheduling status
12WebTMA-2 Ki 5-HT2A binding affinity nM value receptor53Specific binding affinity data for TMA-2
13Web - DEA, Canada, UKTMA-2 US DEA Schedule I status44Confirms legal status across major jurisdictions
14WebTMA-2 SMILES InChIKey CAS32Chemical structure data for TMA-2
15Web - Erowid/Historical sourcesTMA-2 Shulgin history discovery 1962 196432Historical synthesis and discovery narrative
47 claims by section — every cited sentence, checked against its source
safety11 · 7 ok
  • Tolerance develops rapidly — consistent with the well-characterized mechanism of 5-HT₂A receptor downregulation in the frontal cortexsupported

    5-HT2A receptor downregulation (not 5-HT2C) is the mechanism of tolerance to hallucinogenic DOI; class-level mechanism relevant to TMA-2. pmid:10435391

  • Tolerance develops rapidly — consistent with the well-characterized mechanism of 5-HT₂A receptor downregulation in the frontal cortexsupported

    5-HT2AR downregulation in frontal cortex. Tolerance mechanism independent of beta-arrestin-2. acschemneuro.2c00170

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Cross-tolerance with all classical serotonergic psychedelics — including LSD, psilocybin, mescaline, and other DOx compounds — is expected based on their shared 5-HT₂A mechanism.supported

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

  • TMA-2's minimal monoamine transporter activity makes direct serotonin release amplification less likely than with MDMA or amphetaminesupported

    Methoxylated phenethylamines (including TMA-2, 2C-I, 2C-E, 2C-C) had minimal effects on monoamine transport compared to stimulants. pmid:17223101

  • However, potent 5-HT₂A agonism could synergize with MAO inhibition to produce serotonergic toxicitysupported

    Evaluates serotonin toxicity risks between serotonergic psychedelics and SSRIs/MAOIs. s00213-021-05876-x

  • Claim in safety — inconclusiveinconclusiveworking →

  • CYP2D6 substrates may be affected by TMA-2's competitive CYP2D6 inhibitionsupported

    Interactions with CYP2D6 substrates are possible but unlikely at therapeutic concentrations. j.toxlet.2008.09.014

  • Concurrent MAOI use is contraindicated due to theoretical serotonin syndrome risk.supported

    Evaluates serotonin toxicity risks between serotonergic psychedelics and SSRIs/MAOIs. s00213-021-05876-x

pharmacology10 · 5 ok
  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • TMA-2 exerts its psychedelic effects primarily through agonism at the serotonin 5-HT₂A receptorsupported

    Receptor binding affinities determined at 5-HT1A, 5-HT2A, 5-HT2C, TAAR1, alpha-adrenergic, D2 and monoamine transporters. Amphetamine derivatives Ki=61-4400 nM at 5-HT2A; preference over 5-HT1A and 5-HT2C. fphar.2019.01423

  • TMA-2 exerts its psychedelic effects primarily through agonism at the serotonin 5-HT₂A receptorsupported

    TMA-2 at low doses increases locomotor activity in C57BL/6J mice. Effect mediated by 5-HT2A receptor activation. j.neuropharm.2013.01.014

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • TMA-2 exerts minimal influence on monoamine reuptake and release in rat brain synaptosomes, distinguishing it mechanistically from stimulant amphetamines such as amphetamine and MDMAsupported

    TMA-2 and TMA-6 slightly influence reuptake and release of dopamine, 5-HT, and norepinephrine in rat brain synaptosomes. Methoxylated phenethylamines (including TMA-2, 2C-I, 2C-E, 2C-C) had minimal effects on monoamine transport compared to stimulants. pmid:17223101

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • CYP2D6 is the primary cytochrome P450 isoenzyme responsible for O-demethylation of TMA-2supported

    CYP2D6 is the sole CYP isoenzyme involved in O-demethylation of TMA-2 and related compounds. j.toxlet.2008.09.014

  • TMA-2 acts as a non-mechanism-based competitive inhibitor of CYP2D6, with Ki values of 7.1–296 μM in recombinant CYP2D6 and 2.7–19.9 μM in pooled human liver microsomes — substantially weaker than potent CYP2D6 inhibitors such as quinidine (Ki = 0.0092 μM).supported

    TMA-2 is a non-mechanism-based competitive inhibitor of CYP2D6 with Ki 7.1-296 microM (recombinant), 2.7-19.9 microM (HLM). j.toxlet.2008.09.014

  • Claim in pharmacology — not_supportednot supportedworking →

pharmacokinetic-detail7 · 6 ok
  • CYP2D6 is the principal cytochrome P450 isoform mediating O-demethylation of TMA-2supported

    CYP2D6 is the sole CYP isoenzyme involved in O-demethylation of TMA-2 and related compounds. j.toxlet.2008.09.014

  • Claim in pharmacokinetic-detail — inconclusiveinconclusiveworking →

  • TMA-2 is a non-mechanism-based competitive inhibitor of CYP2D6:supported

    TMA-2 is a non-mechanism-based competitive inhibitor of CYP2D6 with Ki 7.1-296 microM (recombinant), 2.7-19.9 microM (HLM). j.toxlet.2008.09.014

  • Standard ELISA immunoassay kits (amphetamine/MDMA panels) cannot reliably detect TMA-2 at concentrations up to 10,000 ng/mLsupported

    Standard immunoassay kits cannot reliably detect TMA-2 and 29 other amphetamine designer drugs at concentrations up to 10,000 ng/mL. Specialized confirmatory methods required for forensic detection. bkw060

  • Definitive identification requires GC/MS or LC-MS/MS methodssupported

    GC/MS STA procedure detects TMA-2 at common user doses in rat urine. pmid:16810708

  • Definitive identification requires GC/MS or LC-MS/MS methodssupported

    Validated LC-MS method for simultaneous quantification of TMA, TMA-2, and TMA-6 in human urine. j.jchromb.2008.03.027

  • Comprehensive reviews of analytical approaches for 2,5-dimethoxyamphetamines in biological matrices are available.supported

    Comprehensive review of analytical methods for DOx amphetamines and 2C-x phenethylamines in blood, urine, hair and other biological matrices. Reviews GC-MS and LC-MS methods. s11419-022-00638-6

comparative-pharmacology5 · 2 ok
  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Unlike amphetamine and MDMA, TMA-2 produces minimal monoamine reuptake inhibition or release in rat brain synaptosomessupported

    TMA-2 and TMA-6 slightly influence reuptake and release of dopamine, 5-HT, and norepinephrine in rat brain synaptosomes. Methoxylated phenethylamines (including TMA-2, 2C-I, 2C-E, 2C-C) had minimal effects on monoamine transport compared to stimulants. pmid:17223101

  • Drug discrimination studies in rats trained on DOM demonstrate cross-substitution with TMA isomers, with the 2,4-dimethoxy pattern identified as important for discriminative stimulus generalization within this classsupported

    DOM-stimulus generalization in rat drug discrimination with TMA isomers. 2,4-dimethoxy pattern important for activity. pmid:6965276

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

receptor-pharmacology5 · 3 ok
  • All receptor data from Kolaczynska et al. (2019) unless otherwise notedsupported

    Receptor binding affinities determined at 5-HT1A, 5-HT2A, 5-HT2C, TAAR1, alpha-adrenergic, D2 and monoamine transporters. fphar.2019.01423

  • Monoamine transporter data from Nagai et al. (2007).supported

    TMA-2 and TMA-6 slightly influence reuptake and release of dopamine, 5-HT, and norepinephrine in rat brain synaptosomes. pmid:17223101

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

  • Specific binding data at alpha-adrenergic and D₂ receptors for TMA-2 were not extractable from available published data, though the Kolaczynska et al. panel notes weak activity at non-5-HT₂ targets for the DO-OCH₃ (amphetamine series) compoundsupported

    Receptor binding affinities determined at 5-HT1A, 5-HT2A, 5-HT2C, TAAR1, alpha-adrenergic, D2 and monoamine transporters. Amphetamine derivatives Ki=61-4400 nM at 5-HT2A; preference over 5-HT1A and 5-HT2C. fphar.2019.01423

summary4 · 1 ok
  • Claim in summary — inconclusiveinconclusiveworking →

  • Claim in summary — inconclusiveinconclusiveworking →

  • It is essentially inactive at 5-HT₁A (Ki ≈ 46,400 nM) and exerts minimal monoamine transporter activity, distinguishing it mechanistically from stimulant amphetamines.supported

    Methoxylated phenethylamines (including TMA-2, 2C-I, 2C-E, 2C-C) had minimal effects on monoamine transport compared to stimulants. pmid:17223101

  • Claim in summary — inconclusiveinconclusiveworking →

neuroscience3 · 3 ok
  • The following mechanistic framework is inferred from the broader serotonergic psychedelic class and from TMA-2's confirmed 5-HT₂A agonism.supported

    Receptor binding affinities determined at 5-HT1A, 5-HT2A, 5-HT2C, TAAR1, alpha-adrenergic, D2 and monoamine transporters. Amphetamine derivatives Ki=61-4400 nM at 5-HT2A; preference over 5-HT1A and 5-HT2C. fphar.2019.01423

  • The following mechanistic framework is inferred from the broader serotonergic psychedelic class and from TMA-2's confirmed 5-HT₂A agonism.supported

    TMA-2 at low doses increases locomotor activity in C57BL/6J mice. Effect mediated by 5-HT2A receptor activation. j.neuropharm.2013.01.014

  • TMA-2's confirmed locomotor hyperactivity in mice, blocked by the selective 5-HT₂A antagonist M100907, confirms that its behavioral effects operate through the same 5-HT₂A-dependent pathwaypartially supported

    TMA-2 at low doses increases locomotor activity in C57BL/6J mice. Effect mediated by 5-HT2A receptor activation. M100907 (5-HT2A antagonist) blocked the hyperactivity induced by mescaline and TCB-2. j.neuropharm.2013.01.014

chemistry1 · 1 ok
  • TMA-2 is the 4-methoxy member of the DOx series (also designated DO-OCH₃ or DOMeO), a family of 4-substituted 2,5-dimethoxyamphetamines within the broader class of substituted phenethylaminessupported

    SAR context for the DOx class. Background: 2,4,5-Trimethoxyamphetamine (TMA-2) is a potent psychedelic compound. fphar.2019.01423

history1 · 0 ok
  • Claim in history — not_supportednot supportedworking →

3Sources

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

Sources
yearsourcetierstatusfeeds
20242,4,5-Trimethoxyamphetamine (TMA-2) product listingCayman Chemicalurl:7987de30028c3c5aweakconsumedcited only
20242,4,5-Trimethoxyamphetamine chemical data (NCATS Inxight Drugs)National Center for Advancing Translational Sciencesurl:ab3c5688f340f913weakconsumedcited only
2023Analysis of 2,5-dimethoxy-amphetamines and 2,5-dimethoxy-phenethylamines aiming their determination in biological matrices: a review.Nieddu M, Baralla E, Sodano F, Boatto G · Forensic Toxicologydoi:10.1007/s11419-022-00638-6moderateconsumed1 section
2022Serotonin toxicity of serotonergic psychedelicsMalcolm B, Thomas K · Psychopharmacologydoi:10.1007/s00213-021-05876-xmoderateconsumed1 section
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
2020Investigation of the 2,5-Dimethoxy Motif in Phenethylamine Serotonin 2A Receptor AgonistsMarcher-Rørsted E, Halberstadt AL, Klein AK, Chatha M, Jademyr S, Jensen AA, Kristensen JL · ACS Chemical Neurosciencedoi:10.1021/acschemneuro.0c00129moderateconsumed2 sections
2019Comparison of the behavioral effects of mescaline analogs using the head twitch response in miceHalberstadt AL, Chatha M, Chapman SJ, Brandt SD · Journal of Psychopharmacologydoi:10.1177/0269881119826610moderateconsumed2 sections
2019Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines.Kolaczynska KE, Luethi D, Trachsel D, Hoener MC, Liechti ME · Frontiers in Pharmacologydoi:10.3389/fphar.2019.01423moderateconsumed6 sections
2016ELISA Detection of 30 New Amphetamine Designer Drugs in Whole Blood, Urine and Oral Fluid using Neogen Amphetamine and Methamphetamine/MDMA KitsNieddu M, Burrai L, Baralla E, Pasciu V, Varoni MV · Journal of Analytical Toxicologydoi:10.1093/jat/bkw060moderateconsumed1 section
2013Role of the 5-HT2A receptor in the locomotor hyperactivity produced by phenylalkylamine hallucinogens in miceHalberstadt AL, Powell SB, Geyer MA · Neuropharmacologydoi:10.1016/j.neuropharm.2013.01.014moderateconsumed2 sections
20082,5-Dimethoxyamphetamine-derived designer drugs: studies on the identification of cytochrome P450 (CYP) isoenzymes involved in formation of their main metabolites and on their capability to inhibit CYP2D6.Ewald AH, Maurer HH · Toxicology Lettersdoi:10.1016/j.toxlet.2008.09.014moderateconsumed3 sections
2008LC-MS analysis of trimethoxyamphetamine designer drugs (TMA series) from urine samplesNieddu M, Boatto G, Pirisi MA, Azara E, Marchetti M · Journal of Chromatography Bdoi:10.1016/j.jchromb.2008.03.027moderateconsumed3 sections
2007The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain.Nagai F, Nonaka R, Satoh Hisashi Kamimura K · European journal of pharmacologypmid:17223101moderateconsumed5 sections
2006Designer drug 2,4,5-trimethoxyamphetamine (TMA-2): studies on its metabolism and toxicological detection in rat urine using gas chromatographic/mass spectrometric techniquesEwald AH, Fritschi G, Maurer HH · Journal of Mass Spectrometrypmid:16810708moderateconsumed2 sections
2003Council Decision 2003/847/JHA concerning control measures and criminal sanctions in respect of the new synthetic drugs 2C-I, 2C-T-2, 2C-T-7 and TMA-2Council of the European Unionurl:0a368bf5af6afc97weakconsumedcited only
2003Report on the risk assessment of TMA-2 (EMCDDA, 2003)European Monitoring Centre for Drugs and Drug Addictionurl:b351a6508b82d88bweakconsumedcited only
1999Mechanism of tolerance development to 2,5-dimethoxy-4-iodoamphetamine in rats: down-regulation of the 5-HT2A, but not 5-HT2C, receptorSmith RL, Barrett RJ, Sanders-Bush E · Psychopharmacologypmid:10435391moderateconsumed1 section
1982Comparison of behavioral properties of di- and tri-methoxyphenylisopropylaminesGlennon RA, Young R · Pharmacology, Biochemistry and Behaviorpmid:6965276moderateconsumed1 section
—Searched ClinicalTrials.gov for "TMA-2 trimethoxyamphetamine" — no resultsabsenceno results—

4Docket

one filing per activity — decisions, correspondence, reports

  1. 0012026-04-26revisionRevision 1

    Initial LLM generation (v5 pipeline, wiki)

    psx:substance/tma-2/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 · 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 · cardiovascular
    • contraindication · cardiovascular
    • contraindication · other
    • contraindication · pregnancy_breastfeeding
    • contraindication · neurological
    • contraindication · other
    psx:substance/tma-2/proposal/dose_tier/d4539385-819a-4b2c-9bad-c2d651aba79c
  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 20:34Revision 1current
info_card9e851aabcee734b89a558c95…2026-10-19 20:34Revision 1current
emergency3f0909c25c714d225b4bb3e3…2026-09-04 04:32Revision 1superseded2026-10-19
info_card9135e62bde4300d027603fd6…2026-09-04 04:32Revision 1superseded2026-10-19
notice77dd343fe8623e9da9c6bf57…2026-09-04 04:32Revision 1current