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Methallylescaline

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

6Node page

what any key link opens

psx:substance/methallylescaline/issue/notice@53ffc98bc5c1

issue2026-10-19recordcurrent

derived from · upstream

  • derived_fromRevision 1psx:substance/methallylescaline/version/1

feeds · downstream

  • invalidated_byIssued noticepsx:substance/methallylescaline/issue/notice@64878b43a1d2

Closure of psx:substance/methallylescaline/issue/notice@53ffc98bc5c1: 36 upstream, 84 downstream.

psx:substance/methallylescaline/issue/notice@53ffc98bc5c1
├─ derived_from  version/1  Revision 1
  ├─ used  src/doi:10.3389/fphar.2021.794254  Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related Amphetamines
  ├─ used  src/url:5790d91cda96f74c  NDEWS Weekly Briefing Issue 181: Methallylescaline alert
  ├─ used  src/doi:10.1038/s41398-024-03116-2  Acute dose-dependent effects of mescaline in a double-blind placebo-controlled study in healthy subjects
  ├─ used  src/url:2949b4df42a1d050  A Trip to the Hospital (Erowid Experience #105249)
  ├─ used  src/doi:10.1124/pr.115.011478  Psychedelics
  ├─ used  src/doi:10.1021/acschemneuro.2c00170  Tolerance and Cross-Tolerance among Psychedelic and Nonpsychedelic 5-HT2A Receptor Agonists in Mice
  ├─ used  src/doi:10.5478/MSL.2018.9.3.86
  ├─ used  src/url:c39d07680fec24ab  NDEWS Web Monitoring Alert: Online mentions of Methallylescaline
  ├─ used  src/doi:10.1007/7854_2017_475  Chemistry and Structure-Activity Relationships of Psychedelics.
  ├─ used  src/doi:10.1038/s41386-023-01607-2  Comparative acute effects of mescaline, lysergic acid diethylamide, and psilocybin in a randomized, double-blind, placebo-controlled cross-over study in healthy participants
  ├─ used  src/doi:10.3389/fphar.2025.1703480  Receptor interaction profiles of 4-alkoxy-2,6-dimethoxyphenethylamines (psi derivatives) and related amphetamines
  ├─ used  src/doi:10.1016/j.biopha.2021.112295  A retrospective analysis of the 'Neverending Trip' after administration of a potent full agonist of 5-HT2A receptor - 25I-NBOMe
  ├─ used  src/doi:10.1007/s00213-021-05876-x  Serotonin toxicity of serotonergic psychedelics
  ├─ derived_from  gen/67d65d9b-ce6c-4414-a96d-5a627ed6d23b  Generation — pipeline-v5
  ├─ generated_by  pub/68ed9fe4-733a-4bbf-adce-62824267c4aa  Publication — backfill
    ├─ used  search/0b8198ac-162d-4f5a-84e8-1290ff0d7983  Searched PubChem for "methallylescaline"
    ├─ used  search/5a2f12d0-36f8-4e7b-9ca0-c4963f357664  Searched PubMed for "methallylescaline MAL phenethylamine psychedelic"
    ├─ used  search/b2e7b29a-11f1-4af0-ae81-ba700817f693  Searched OpenAlex for "methallylescaline pharmacology psychedelic"
    ├─ used  search/3b1492fe-ec6b-43b8-a0cd-963e969e115c  Searched PubMed for "mescaline analog 4-alkoxy substitution serotonin receptor psychedelic potency"
    ├─ used  search/c68341b1-dc93-4d25-8700-9206e1888a25  Searched WebSearch for "methallylescaline MAL pharmacology effects dose PiHKAL Shulgin"
    ├─ used  search/b3438b7f-9b69-4c20-b13e-25cf98fd2ab8  Searched Erowid PiHKAL for "MAL methallylescaline PiHKAL entry #99"
    ├─ used  search/c81de31e-4a90-4de1-adad-5e671961c0b0  Searched PMC/Frontiers in Pharmacology for "Kolaczynska 2021 MAL methallylescaline receptor data"
    ├─ used  search/ddb896cb-a750-4f82-955e-35a21836a740  Searched WebSearch for "methallylescaline MAL legal status scheduling UK US EU"
    ├─ used  search/98a06847-daf7-4065-9161-b835b8f3e88f  Searched WebSearch for "NDEWS methallylescaline 2024 alert"
    ├─ used  search/c2ce0d31-4242-4e02-b805-2441cd9d0086  Searched WebSearch for "methallylescaline synthesis CAS 207740-41-8 SMILES"
    ├─ used  search/5c15eee7-7c18-4990-a1b0-5653f126f0c1  Searched ClinicalTrials.gov for "methallylescaline mescaline analog"
    ├─ used  search/5fe9fa28-c385-4d62-b5c2-79683eaefdf8  Searched PubMed for "get_pubmed_article PMID 30789291"
    ├─ used  search/b289a492-2894-4c8a-b652-11139f23f1fa  Searched PubMed for "get_pubmed_article PMID 39587436 39349427 37231080"
    ├─ used  search/3b40e35d-54d5-4829-a35e-0be8d1939891  Searched Erowid for "methallylescaline hospital trip report"
    ├─ used  search/b71cff27-7919-4df2-9cf0-72ff04e01390  Searched PubMed for "serotonin toxicity serotonergic psychedelics drug interaction SSRI MAOI"
    ├─ used  search/874e3243-597d-44f4-ac32-a2bc80aa88b9  Searched Multiple sources for "methallylescaline dose duration cross-reference PiHKAL vs Kolaczynska 2021 vs seed data"
    ├─ used  search/95400306-219c-4a9f-91b5-bab68efdef45  Searched PMC/Frontiers in Pharmacology for "Kolaczynska 2021 MAL allylescaline mescaline comparative data"
    ├─ used  search/b79c3831-bbd4-496f-a014-f477e344ef25  Searched Erowid for "methallylescaline hospital trip case report 130mg"
    ├─ used  search/76ee9435-1900-45a6-91d3-049bb2050118  Searched PubMed for "mescaline human dose subjective effects clinical controlled crossover study"
    └─ used  search/200e724b-efd3-4def-8d1d-5fba8a4a4604  Searched WebSearch for "methallylescaline allylescaline escaline potency comparison mescaline 4-alkoxy PiHKAL"
├─ invalidated_by  issue/notice@64878b43a1d2  Issued notice
  ├─ derived_from  issue/info_card@263906c2ff10  Issued info_card
  ├─ derived_from  issue/emergency@3f0909c25c71  Issued emergency
  ├─ derived_from  issue/info_card@37154db2304e  Issued info_card
  ├─ derived_from  issue/emergency@c15c760aabf6  Issued emergency
    ├─ used  claim/116047d8-6625-4c36-920a-d451cf3824a0  Claim in summary — partially_supported
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    ├─ used  claim/a3953045-be3b-4137-b195-c401e9ddc4fb  Claim in summary — supported
    ├─ used  claim/b3f7859d-1bdd-4f9b-9fd3-c743f15e7ba3  Claim in pharmacology — supported
    ├─ used  claim/a61a1a0e-074b-4236-81f2-c4dab319ed45  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/b8d70709-f922-464b-9bb7-2a81db47b68c  Claim in pharmacology — supported
    ├─ used  claim/8f1c8b00-1eba-4a21-9514-cb80ba110938  Claim in pharmacology — inconclusive  working
    ├─ used  claim/d8e4b853-9867-49e5-a30f-0a39230da918  Claim in pharmacology — inconclusive  working
    ├─ used  claim/c60237bf-7364-4e7b-9642-68e7e291a850  Claim in pharmacology — inconclusive  working
    ├─ used  claim/16f9aee5-ac49-4d8b-ade5-e98f83798be0  Claim in pharmacology — supported
    ├─ used  claim/698b26f9-c58a-42a1-b28e-926c53e65376  Claim in safety — inconclusive  working
    ├─ used  claim/d1713941-2218-4860-bf54-1a1ce49538c6  Claim in safety — inconclusive  working
    ├─ used  claim/386ba855-5eeb-4c99-819d-fb6ee72512ce  Claim in safety — inconclusive  working
    ├─ used  claim/23da8a65-6d48-41a7-8f46-064d2d2fb721  Claim in safety — inconclusive  working
    ├─ used  claim/7bbdc3d8-115a-4aa4-a702-9a8a32064e06  Claim in history — inconclusive  working
    ├─ used  claim/8659df6a-14b4-4f08-b2b0-2d6b1949bbe9  Claim in chemistry — supported
    ├─ used  claim/e47a15e2-32a5-48ff-be89-55e5b3fa7a37  Claim in chemistry — inconclusive  working
    ├─ used  claim/b35bbdea-f4ba-4577-95ba-55176820a290  Claim in receptor-pharmacology — supported
    ├─ used  claim/7beab31f-0704-4029-bcce-8ccb8d152b06  Claim in receptor-pharmacology — supported
    ├─ used  claim/06c31b69-cd85-40c1-b815-af7e73ccd3dd  Claim in receptor-pharmacology — inconclusive  working
    ├─ used  claim/f832fb97-8044-4880-8761-05f774bac258  Claim in receptor-pharmacology — supported
    ├─ used  claim/c486760b-e879-4bda-bf05-60379fc0dcf8  Claim in comparative-pharmacology — supported
    ├─ used  claim/a3ed498e-c345-4911-90d2-bdfefdc169cd  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/120dabfa-1e80-4999-a721-678db050d09b  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/9091b12b-0c8e-43fa-8bd3-f9de9521e9fc  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/17556f68-b5b2-4a1f-afa5-ad39519f3f55  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/eb8449a9-ef3a-4156-acce-c0be4a332d83  Claim in neuroscience — supported
    ├─ used  claim/3d234f63-04a8-47f8-9a74-7da84b916fab  Claim in summary — supported
    ├─ used  claim/1928b05e-b600-41d7-bd04-dcde0b21e805  Claim in pharmacology — supported
    ├─ used  claim/976802ae-db4f-4797-a4cf-0f8b8d9357f0  Claim in pharmacology — supported
    ├─ used  claim/e8f2138d-7204-4268-8069-b4a18796b521  Claim in safety — inconclusive  working
    ├─ used  claim/577a5a41-6c78-4a37-b5a3-fecef20ec40d  Claim in safety — supported
    ├─ used  claim/db5a3771-b3ae-4d66-91af-3f7a77341372  Claim in safety — inconclusive  working
    ├─ used  claim/198371d4-4a37-4b2e-888c-ae2b362fb43d  Claim in pharmacokinetic-detail — supported
    ├─ used  claim/92ab5be1-5428-4d30-87c2-19be6966c368  Claim in clinical-evidence — supported
    ├─ used  claim/ab07203a-eddc-4119-9d82-2ae7dc500ba3  Claim in comparative-pharmacology — supported
    ├─ used  claim/d5f331ef-5bff-4ff0-bc0a-30c67e7206bc  Claim in comparative-pharmacology — supported
    ├─ used  claim/25b5a1c9-4a3d-4e0d-9f2a-b9f52d623787  Claim in summary — supported
    ├─ used  claim/c0a818d4-a86d-4166-a91b-eec5e5008325  Claim in pharmacology — supported
    ├─ used  claim/e7c15998-21fa-4c1a-9e1b-5fe899620604  Claim in safety — inconclusive  working
    ├─ used  claim/7bb90e0d-7b50-4f77-a280-c21a25fe2362  Claim in safety — supported
    ├─ used  claim/3faa8734-8c39-4dfd-969b-4d3860f6e295  Claim in safety — inconclusive  working
    ├─ used  claim/a9920483-f807-4a9b-82cd-71d999b0960f  Claim in neuroscience — inconclusive  working
    ├─ used  claim/9eb8bacb-8489-4f0a-be91-72b61d7f9373  Claim in summary — supported
    ├─ used  claim/33c35f53-96cf-40e4-84aa-c468c8d8c41d  Claim in safety — inconclusive  working
    ├─ used  claim/650b8906-9b48-4bcf-a9ee-245f12ef0d0b  Claim in safety — partially_supported
    ├─ used  claim/912c2166-6931-4141-a680-96772c9fdc67  Claim in comparative-pharmacology — supported
    ├─ used  claim/f56ea787-2749-45f4-80dc-0d9e2a3e5550  Claim in pharmacology — supported
    ├─ used  claim/ba61473c-84a4-455c-959a-a438f88fa816  Claim in pharmacology — supported
    ├─ used  claim/88e820b4-c5de-4579-919c-55d8d71be8e8  Claim in pharmacology — supported
    ├─ used  claim/f2bb7e62-afac-42b2-a592-be7277c79511  Claim in safety — supported
    ├─ used  claim/297502ce-0f55-43b6-9e53-2c010de0c478  Claim in safety — supported
    ├─ used  claim/a751546e-9b0d-4035-80a6-68f138ae6186  Claim in history — supported
    ├─ used  claim/ffdf8f9c-21fe-4815-ba08-abae919da2f0  Claim in chemistry — inconclusive  working
    ├─ used  claim/d95798b4-6cf0-45ca-bb3a-d4d7ffdb2845  Claim in pharmacokinetic-detail — supported
    ├─ used  claim/db7e793b-f948-4a69-b4b5-84034165861b  Claim in pharmacokinetic-detail — supported
    ├─ used  claim/9d7c1e1c-268c-46d6-95bd-3f0f8af4cd7d  Claim in pharmacokinetic-detail — supported
    ├─ used  claim/4fcebc06-31fd-4ccd-ac6a-ea8f3f70e525  Claim in pharmacokinetic-detail — supported
    ├─ used  claim/43d81859-52ad-4112-a05a-fe4b43709766  Claim in chemistry — inconclusive  working
    ├─ used  claim/a239a9ec-fbcd-4a16-a7b7-568ebf6072c5  Claim in pharmacology — inconclusive  working
    ├─ used  claim/c0361a11-eb41-498d-86f3-33e6179f38be  Claim in comparative-pharmacology — supported
    ├─ used  claim/832c25e8-a432-4509-a8f3-2cf5b59e3885  Claim in pharmacokinetic-detail — inconclusive  working
    ├─ used  claim/13907816-3084-47af-9726-a77561773b1b  Claim in clinical-evidence — supported
    ├─ used  claim/3fa2796d-2c18-4786-81f4-8f20f2aca96b  Claim in comparative-pharmacology — supported
    ├─ used  claim/b72f85fb-d847-46d0-b6ab-dbd2286136f6  Claim in comparative-pharmacology — supported
    ├─ used  claim/79c4bf8d-8aa2-48cf-965b-f0d8d5a7d0fd  Claim in safety — supported
    ├─ used  claim/e8e93577-cdf5-4ace-af2e-1abc32eeca3d  Claim in safety — supported
    ├─ used  claim/66aa2670-cc72-460a-9fbb-8c885ede36cc  Claim in safety — supported
    ├─ used  claim/0e7cc204-2223-4f74-a1e7-f94861eb10ce  Claim in safety — supported
      ├─ informed_by  section/summary.full@1
      ├─ informed_by  section/pharmacology.full@1
      ├─ informed_by  section/comparative-pharmacology.full@1
      ├─ informed_by  section/safety.full@1
      ├─ informed_by  section/history.full@1
      ├─ informed_by  section/chemistry.full@1
      ├─ informed_by  section/receptor-pharmacology.full@1
      ├─ informed_by  section/neuroscience.full@1
      ├─ informed_by  section/pharmacokinetic-detail.full@1
      └─ informed_by  section/clinical-evidence.full@1

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