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Methallylescaline

3,5-dimethoxy-4-(2-methylallyloxy)phenethylamine

6Node page

what any key link opens

psx:substance/methallylescaline/value/toxicity@1

valuereferenced by edges — no row of its own

derived from · upstream

  • derived_fromtoxicitypsx:substance/methallylescaline/proposal/toxicity/f9c6f6f1-cd7e-4092-9d56-bdfac5eac2fd

feeds · downstream

none recorded

Closure of psx:substance/methallylescaline/value/toxicity@1: 1 upstream, 0 downstream.

psx:substance/methallylescaline/value/toxicity@1
└─ derived_from  proposal/toxicity/f9c6f6f1-cd7e-4092-9d56-bdfac5eac2fd  toxicity

indented by distance from this node, not by parentage

1Provenance card

the boundary, as counts

Sources

1310 with DOI

4 strong · 4 moderate · 5 weak

Compilations

12026-05-11T05:55:59.119Z

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

Decisions

30last ruled 2026-06-04

0 awaiting a ruling

Issued documents

62026-10-19T20:32:50.315Z

notice · info card · emergency

Searches

201 with no results

queries and counts on the build

Claims checked

6943 supported

43 supported · 26 not

Correspondence

0received

consent field ships in Phase 4

Edges

218

derivations recorded for this entity

Complete over 13 sources, 1 compilation, and 30 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/methallylescaline/archive

2Build

one panel per compilation run

generation run 2026-05-11

65 min completedmodel pipeline-v5plan not recordedrun/6c1de0ae…

Selection

results seen74
selected by the model17
consumed as sources13

Verification

claims checked69
supported41
partially supported2
not supported0
inconclusive26
  • record
  • seen / partial
  • working

The model's own caveats

4 further caveats recorded as free text — readable on the working page

Reproduce

inputs
13 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
20 searches — query, source, results, what was kept and why
20 searches for this run
#sourcequeryseenkeptrationale
1PubChemmethallylescaline11Only result; confirms chemical identity data from seed brief.
2PubMedmescaline analog 4-alkoxy substitution serotonin receptor psychedelic potency11Direct comparison of mescaline analog potency including escaline family.
3PubMedmethallylescaline MAL phenethylamine psychedelic1——
4ClinicalTrials.gov · absencemethallylescaline mescaline analog0——
5WebSearchNDEWS methallylescaline 2024 alert10——
6OpenAlexmethallylescaline pharmacology psychedelic6——
7Erowid PiHKALMAL methallylescaline PiHKAL entry #991——
8WebSearchmethallylescaline synthesis CAS 207740-41-8 SMILES10——
9WebSearchmethallylescaline MAL pharmacology effects dose PiHKAL Shulgin104Multiple converging sources confirm PiHKAL origin and 2021 pharmacology paper.
10PMC/Frontiers in PharmacologyKolaczynska 2021 MAL methallylescaline receptor data1——
11WebSearchmethallylescaline MAL legal status scheduling UK US EU10——
12Erowidmethallylescaline hospital trip report11—
13PubMedget_pubmed_article PMID 3078929111—
14Multiple sourcesmethallylescaline dose duration cross-reference PiHKAL vs Kolaczynska 2021 vs seed data33—
15PubMedget_pubmed_article PMID 39587436 39349427 3723108033—
16PubMedserotonin toxicity serotonergic psychedelics drug interaction SSRI MAOI11—
17WebSearchmethallylescaline allylescaline escaline potency comparison mescaline 4-alkoxy PiHKAL10——
18PubMedmescaline human dose subjective effects clinical controlled crossover study2——
19PMC/Frontiers in PharmacologyKolaczynska 2021 MAL allylescaline mescaline comparative data12—
20Erowidmethallylescaline hospital trip case report 130mg1——
69 claims by section — every cited sentence, checked against its source
safety18 · 9 ok
  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Nausea and vomiting are prominent adverse effects, particularly at higher doses, consistent with the mescaline classsupported

    Nausea and emesis frequent at 800 mg s41398-024-03116-2

  • Claim in safety — inconclusiveinconclusiveworking →

  • Hallucinogen persisting perception disorder (HPPD) — persistent visual disturbances following psychedelic use have been documented with potent 5-HT₂A agonist novel psychoactive substances. No MAL-specific HPPD cases have been published, but the risk is presumed to exist on pharmacological grounds.supported

    5-HT2A receptor agonists (e.g. 25I-NBOMe) pose risks of acute intoxication and long-term adverse effects including HPPD, derealization, and depersonalization j.biopha.2021.112295

  • MAL, consistent with all characterized serotonergic psychedelics, is not habit-forming and carries no physical dependence liabilitysupported

    Generally considered physiologically safe and do not lead to dependence or addiction pr.115.011478

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Cross-tolerance extends to other 5-HT₂A agonists including LSD, psilocybin, mescaline, and DOx-series compounds.partially supported

    Cross-tolerance between DOI and LSD but not nonpsychedelic 5-HT2AR agonist lisuride acschemneuro.2c00170

  • Monoamine oxidase inhibitors (MAOIs). The combination of MAOIs with serotonergic psychedelics carries risk of serotonin toxicitysupported

    Evaluates drug-drug interaction risks and serotonin toxicity between psychedelic serotonergic substances and SSRIs/MAOIs s00213-021-05876-x

  • SSRIs and SNRIs. Selective serotonin reuptake inhibitors may attenuate psychedelic effects through chronic 5-HT₂A receptor downregulation and can, in some combinations, raise serotonin toxicity risksupported

    Evaluates drug-drug interaction risks and serotonin toxicity between psychedelic serotonergic substances and SSRIs/MAOIs s00213-021-05876-x

  • CYP2D6 and CYP3A4 inhibitors. MAL is metabolized by CYP2D6, CYP2J2, CYP1A2, and CYP3A4supported

    CYP2D6, CYP2J2, CYP1A2, and CYP3A4 enzymes responsible msl.2018.9.3.86

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Concurrent MAOI use. Risk of serotonin toxicity.supported

    serotonin toxicity between psychedelic serotonergic substances and SSRIs/MAOIs s00213-021-05876-x

  • Hepatic impairment. MAL is metabolized by multiple CYP enzymes; impaired hepatic function could reduce clearance and increase exposuresupported

    CYP2D6, CYP2J2, CYP1A2, and CYP3A4 enzymes responsible msl.2018.9.3.86

pharmacology13 · 9 ok
  • In the only published pharmacological characterization, Kolaczynska and colleagues determined a 5-HT₂A binding affinity of Ki = 550 ± 190 nM and a functional activation EC50 of 79 ± 12 nM with 85 ± 5% efficacy relative to serotonin, classifying MAL as a potent full agonist at this targetsupported

    Ki 550±190 nM, EC50 79±12 nM, efficacy 85±5% fphar.2021.794254

  • Near-equivalent affinity at 5-HT₂C (Ki = 520 ± 150 nM) and markedly lower affinity at 5-HT₁A (Ki = 5,100 ± 500 nM) produce a selectivity ratio of approximately 9.3-fold for 5-HT₂A over 5-HT₁A.supported

    5-HT2C Ki 520±150 nM, 5-HT1A Ki 5100±500 nM fphar.2021.794254

  • Activation of 5-HT₂A receptors expressed on the apical dendrites of layer V pyramidal neurons in the prefrontal cortex is the established primary mechanism for serotonergic psychedelic effectssupported

    agonists or partial agonists at brain serotonin 5-HT2A receptors, particularly on apical dendrites of neocortical pyramidal cells in layer V pr.115.011478

  • This mechanism is confirmed by blocking studies: the selective 5-HT₂A antagonist ketanserin attenuates the subjective effects of mescaline in controlled human settings, establishing that 5-HT₂A agonism is both necessary and sufficient for mescaline-class psychedelic activity.supported

    Ketanserin attenuated effects confirming 5-HT2A primary mechanism s41398-024-03116-2

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Mescaline reaches peak plasma concentration (Tmax) at approximately 2 hours after oral administration, with a plasma elimination half-life of approximately 3.5 hourssupported

    Tmax ~2h, t1/2 ~3.5h s41398-024-03116-2

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Total duration ranges from 8–16 hours depending on dose — Shulgin reported 12–16 hours at doses of 40–65 mg, while Kolaczynska and colleagues cite 8–12 hourssupported

    duration 8-12 h fphar.2021.794254

  • The sole published metabolic study employed in vitro incubation of MAL with human hepatocytes, analyzed by liquid chromatography–high resolution mass spectrometry (LC-HRMS)supported

    MAL metabolized... in human hepatocytes... Liquid Chromatography-High Resolution Mass Spectrometry msl.2018.9.3.86

  • The metabolizing enzymes identified are CYP2D6, CYP2J2, CYP1A2, and CYP3A4supported

    CYP2D6, CYP2J2, CYP1A2, and CYP3A4 enzymes responsible msl.2018.9.3.86

  • CYP2D6 inhibitors (fluoxetine, paroxetine, bupropion) and CYP3A4 inhibitors (ketoconazole, grapefruit juice) could increase MAL plasma concentrations through competitive metabolic inhibition.supported

    CYP2D6, CYP2J2, CYP1A2, and CYP3A4 enzymes responsible msl.2018.9.3.86

comparative-pharmacology12 · 7 ok
  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Duration: MAL's total duration (8–16 hours) overlaps with mescaline's (mean 11.1 hours at 500 mg in Ley et al.), though PiHKAL suggests the upper range of MAL may exceed mescaline's typical duration.supported

    Mescaline longest duration (11.1h) s41386-023-01607-2

  • Kolaczynska and colleagues characterized a systematic series of 4-alkoxy-3,5-dimethoxy-phenethylamines, enabling direct comparison of MAL to its structural siblings:supported

    mescaline derivatives including methallylescaline (MAL) at 5-HT2A fphar.2021.794254

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Nausea: Both produce nausea as a prominent adverse effect at higher doses, a consistent feature of the mescaline class.supported

    Nausea and emesis frequent at 800 mg s41398-024-03116-2

  • Clinical data: Mescaline has been characterized in controlled double-blind trials. MAL has none.supported

    Randomized double-blind crossover study in 16 healthy subjects receiving mescaline 100-800 mg s41398-024-03116-2

  • Clinical data: Mescaline has been characterized in controlled double-blind trials. MAL has none.supported

    RCT comparing mescaline (300/500 mg), LSD (100 µg) and psilocybin (20 mg) in 32 healthy participants s41386-023-01607-2

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Cross-tolerance between MAL and tryptamine psychedelics is expected on the basis of shared 5-HT₂A agonism.supported

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

  • A 2025 follow-up study by Kolaczynska and colleagues expanded receptor profiling to psi-derivatives (4-alkoxy-2,6-dimethoxyphenethylamines), providing additional comparative context for the alkoxy-mescaline pharmacological spacesupported

    4-substituted 2,6-dimethoxyphenethylamines and amphetamines compared to 2,4,5- and 3,4,5-substituted analogs fphar.2025.1703480

pharmacokinetic-detail6 · 5 ok
  • Pharmacokinetic table: Oral Tmax (estimated) — Unknown, mescaline Tmax ~2 hours; Plasma half-life — Unknown, mescaline t½ ~3.5 hours; Oral bioavailability — Not determined; Primary metabolizing enzymes — CYP2D6, CYP2J2, CYP1A2, CYP3A4; Identified metabolites — M1–M3 (mono-OH), M4 (di-OH)supported

    Tmax ~2h, t1/2 ~3.5h s41398-024-03116-2

  • Claim in pharmacokinetic-detail — inconclusiveinconclusiveworking →

  • Pharmacokinetic table: Primary metabolizing enzymes — CYP2D6, CYP2J2, CYP1A2, CYP3A4; Identified metabolites — M1–M3 (mono-OH), M4 (di-OH) — all hydroxylation at methallyl moiety; Phase II conjugation — Not observed in vitrosupported

    MAL metabolized to 3 mono-hydroxylated (M1-M3) and 1 di-hydroxylated (M4) metabolite... CYP2D6, CYP2J2, CYP1A2, and CYP3A4 enzymes responsible msl.2018.9.3.86

  • Pharmacokinetic table (duplicate entry): Primary metabolizing enzymes — CYP2D6, CYP2J2, CYP1A2, CYP3A4; Identified metabolites — M1–M3 (mono-OH), M4 (di-OH) — all hydroxylation at methallyl moiety; Phase II conjugation — Not observed in vitrosupported

    MAL metabolized to 3 mono-hydroxylated (M1-M3) and 1 di-hydroxylated (M4) metabolite... CYP2D6, CYP2J2, CYP1A2, and CYP3A4 enzymes responsible msl.2018.9.3.86

  • Kim and colleagues identified four cytochrome P450 isoforms contributing to MAL's oxidative metabolism: CYP2D6, CYP2J2, CYP1A2, and CYP3A4supported

    CYP2D6, CYP2J2, CYP1A2, and CYP3A4 enzymes responsible msl.2018.9.3.86

  • The Kim et al. (2018) study was developed explicitly to support forensic and clinical toxicology screeningsupported

    Framework for forensic toxicology screening msl.2018.9.3.86

summary6 · 5 ok
  • MAL displays approximately six-fold greater 5-HT₂A binding affinity than mescaline (Ki = 550 ± 190 nM vs low-µM range), with an oral duration of 8–16 hours depending on dose, placing it among the longer-acting members of its class.partially supported

    duration 8-12 h fphar.2021.794254

  • Claim in summary — inconclusiveinconclusiveworking →

  • MAL acts as a potent full agonist at the human 5-HT₂A receptor (EC50 = 79 ± 12 nM, 85% efficacy) with near-equal 5-HT₂C affinity (Ki = 520 ± 150 nM) and negligible activity at 5-HT₂B, monoamine transporters, and dopamine D2 receptorssupported

    EC50 79±12 nM, efficacy 85±5%, 5-HT2C Ki 520±150 nM fphar.2021.794254

  • This selectivity profile is consistent with a classical serotonergic psychedelic mechanism, and 5-HT₂A antagonism blocks mescaline-class effects in controlled settings.supported

    Ketanserin attenuated effects confirming 5-HT2A primary mechanism s41398-024-03116-2

  • MAL is not habit-forming and carries no physical dependence liability consistent with its classsupported

    Generally considered physiologically safe and do not lead to dependence or addiction pr.115.011478

  • Tolerance develops rapidly via 5-HT₂A receptor downregulation, with cross-tolerance to other serotonergic psychedelicssupported

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

chemistry4 · 1 ok
  • This places MAL alongside allylescaline (AL, bearing an unsubstituted allyloxy group), escaline (ethyloxy), and proscaline (propyloxy) within a systematic structure-activity series exploring the effect of 4-alkoxy chain length and branching on psychedelic potency and duration.supported

    mescaline derivatives including methallylescaline (MAL) fphar.2021.794254

  • Claim in chemistry — inconclusiveinconclusiveworking →

  • Claim in chemistry — inconclusiveinconclusiveworking →

  • Claim in chemistry — inconclusiveinconclusiveworking →

receptor-pharmacology4 · 3 ok
  • The receptor interaction profile of methallylescaline was characterized in a single comprehensive study by Kolaczynska and colleagues, who tested MAL (compound #32 in their series) across serotonin, dopamine, adrenergic, and trace amine-associated receptor (TAAR) targets using radioligand displacement binding and functional activation assays.supported

    receptor binding profiles (Ki) and functional activation (EC50)... at 5-HT2A, 5-HT2C, 5-HT1A, TAAR1, adrenergic and dopaminergic receptors fphar.2021.794254

  • The 85% efficacy classifies MAL as a full agonist by the conventions of this assay system (referenced to serotonin).supported

    efficacy 85±5% fphar.2021.794254

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

  • This profile predicts classical psychedelic phenomenology without stimulant, empathogenic, or cardiac valvulopathic properties — predictions consistent with the available human subjective reports.supported

    5-HT2A Ki 550±190 nM, EC50 79±12 nM, efficacy 85±5% fphar.2021.794254

clinical-evidence2 · 2 ok
  • The compound's closest pharmacological relative with clinical data is mescaline, for which Klaiber and colleagues published acute dose-dependent effects in healthy participants in a double-blind, placebo-controlled designsupported

    Randomized double-blind crossover study in 16 healthy subjects receiving mescaline 100-800 mg s41398-024-03116-2

  • and Ley and colleagues compared mescaline to LSD and psilocybin in a randomized crossover studysupported

    RCT comparing mescaline (300/500 mg), LSD (100 µg) and psilocybin (20 mg) in 32 healthy participants s41386-023-01607-2

history2 · 1 ok
  • Claim in history — inconclusiveinconclusiveworking →

  • Separately, Kim and colleagues (2018) published the only study of MAL's metabolic fate, identifying four hydroxylated metabolites via in vitro hepatocyte incubation to support forensic detection.supported

    MAL metabolized to 3 mono-hydroxylated (M1-M3) and 1 di-hydroxylated (M4) metabolite in human hepatocytes... Framework for forensic toxicology screening msl.2018.9.3.86

neuroscience2 · 1 ok
  • As a full agonist at cortical 5-HT₂A receptors (EC50 = 79 nM, 85% efficacy), MAL is predicted to engage the same neural mechanisms established for other serotonergic psychedelics:supported

    EC50 79±12 nM, efficacy 85±5% fphar.2021.794254

  • Claim in neuroscience — inconclusiveinconclusiveworking →

3Sources

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

Sources
yearsourcetierstatusfeeds
2025Receptor interaction profiles of 4-alkoxy-2,6-dimethoxyphenethylamines (psi derivatives) and related amphetaminesKolaczynska KE, Trachsel D, Hoener MC, Liechti ME, Luethi D · Frontiers in Pharmacologydoi:10.3389/fphar.2025.1703480moderateconsumed1 section
2024Acute dose-dependent effects of mescaline in a double-blind placebo-controlled study in healthy subjectsKlaiber A, Schmid Y, Becker AM, Straumann I, Erne L, Jelusic A, Thomann J, Luethi D, Liechti ME · Translational Psychiatrydoi:10.1038/s41398-024-03116-2strongconsumed6 sections
2024NDEWS Web Monitoring Alert: Online mentions of MethallylescalineNational Drug Early Warning System (NDEWS), HealthStreeturl:c39d07680fec24abweakconsumedcited only
2024NDEWS Weekly Briefing Issue 181: Methallylescaline alertNational Drug Early Warning System (NDEWS)url:5790d91cda96f74cweakconsumedcited only
2023Comparative acute effects of mescaline, lysergic acid diethylamide, and psilocybin in a randomized, double-blind, placebo-controlled cross-over study in healthy participantsLey L, Holze F, Arikci D, Becker AM, Straumann I, Klaiber A, Coviello F, Dierbach S, Thomann J, Duthaler U, Luethi D, Varghese N, Eckert A, Liechti ME · Neuropsychopharmacologydoi:10.1038/s41386-023-01607-2strongconsumed4 sections
2022A retrospective analysis of the 'Neverending Trip' after administration of a potent full agonist of 5-HT2A receptor - 25I-NBOMeSchetz D, Schetz A, Kocic I · Biomedicine & Pharmacotherapydoi:10.1016/j.biopha.2021.112295weakconsumed1 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.2c00170moderateconsumed3 sections
2021Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related AmphetaminesKolaczynska KE, Luethi D, Trachsel D, Hoener MC, Liechti ME · Frontiers in Pharmacologydoi:10.3389/fphar.2021.794254moderateconsumed8 sections
2018Chemistry and Structure-Activity Relationships of Psychedelics.Nichols DE · Current Topics in Behavioral Neurosciencesdoi:10.1007/7854_2017_475strongconsumed1 section
2018In vitro Metabolism of Methallylescaline in Human Hepatocytes Using Liquid Chromatography-High Resolution Mass SpectrometryKim S, Kim JH, Kim DK, Lee J, In S, Lee HS · Mass Spectrometry Lettersdoi:10.5478/msl.2018.9.3.86weakconsumedcited only
2016PsychedelicsNichols DE · Pharmacological Reviewsdoi:10.1124/pr.115.011478strongconsumed4 sections
2013A Trip to the Hospital (Erowid Experience #105249)Anonymousurl:2949b4df42a1d050weakconsumedcited only
—Searched ClinicalTrials.gov for "methallylescaline mescaline analog" — no resultsabsenceno results—

4Docket

one filing per activity — decisions, correspondence, reports

  1. 0012026-05-11revisionRevision 1

    Initial LLM generation (v5 pipeline, wiki, prose phase)

    psx:substance/methallylescaline/version/1
  2. 0022026-06-04proposal28 value proposals approved together

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

    28 items in this filing

    • contraindication · psychiatric
    • contraindication · other
    • contraindication · neurological
    • contraindication · pregnancy_breastfeeding
    • contraindication · hepatic
    • contraindication · other
    • 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
    • dose_tier · threshold
    • 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
    psx:substance/methallylescaline/proposal/contraindication/d2d87a36-4b73-47b7-83ff-ef50d1a36d66
  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 20:32Revision 1current
info_card37154db2304ebca081bf4cfd…2026-10-19 20:32Revision 1current
notice53ffc98bc5c175e403d133df…2026-10-19 20:32Revision 1current
emergency3f0909c25c714d225b4bb3e3…2026-09-04 04:31Revision 1superseded2026-10-19
info_card263906c2ff10cf7a7c63ae29…2026-09-04 04:31Revision 1superseded2026-10-19
notice64878b43a1d2932a5305f55b…2026-09-04 04:31Revision 1superseded2026-10-19