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Proscaline

3,5-dimethoxy-4-propoxyphenethylamine

6Node page

what any key link opens

psx:substance/proscaline/proposal/dose_tier/b0e5ccc0-4d0e-4e56-8223-78d8117b4dd9

proposal2026-05-03recordapproved

derived from · upstream

none recorded

feeds · downstream

Closure of psx:substance/proscaline/proposal/dose_tier/b0e5ccc0-4d0e-4e56-8223-78d8117b4dd9: 0 upstream, 1 downstream.

psx:substance/proscaline/proposal/dose_tier/b0e5ccc0-4d0e-4e56-8223-78d8117b4dd9
└─ derived_from  value/dose_tier/light@1

indented by distance from this node, not by parentage

1Provenance card

the boundary, as counts

Sources

159 with DOI

2 strong · 9 moderate · 4 weak

Compilations

12026-05-03T11:40:10.708Z

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

Decisions

30last ruled 2026-06-04

0 awaiting a ruling

Issued documents

62026-10-19T20:33:50.756Z

notice · info card · emergency

Searches

202 with no results

queries and counts on the build

Claims checked

4129 supported

29 supported · 12 not

Correspondence

0received

consent field ships in Phase 4

Edges

164

derivations recorded for this entity

Complete over 15 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/proscaline/archive

2Build

one panel per compilation run

generation run 2026-05-03

49 min completedmodel pipeline-v5plan not recordedrun/0344bfd2…

Selection

results seen62
selected by the model25
consumed as sources15

Verification

claims checked41
supported25
partially supported4
not supported2
inconclusive10
  • record
  • seen / partial
  • working

The model's own caveats

none raised on this run

Reproduce

inputs
15 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
1PubChemproscaline11Single entry; confirms molecular identity and provides verified chemical data
2PubMedmescaline head twitch response 5-HT2A potency ED5011Critical methodological paper validating HTR assay's predictive validity for human hallucinogenic potency
3OpenAlexproscaline 3,5-dimethoxy-4-propoxyphenethylamine11Confirmed primary research source; citation graph revealed unrelated related works
4ClinicalTrials.gov · absenceproscaline00No results - confirms absence of clinical trial data for this substance
5PubMedproscaline phenethylamine psychedelic11Only PubMed result directly studying proscaline; highly relevant for pharmacology and SAR
6PubMedmescaline pharmacokinetics metabolism phenethylamine human103Most directly relevant mescaline PK studies; mescaline is the structural parent compound of proscaline
7PubMedmescaline analogs serotonin 5-HT2A receptor binding affinity phenethylamine33Selected papers on 5-HT2A binding of mescaline-class phenethylamines relevant to proscaline's pharmacological class
8ClinicalTrials.gov · absenceproscaline00No trials - confirms absence of formal clinical research
9PubMednew psychoactive substances phenethylamine legal status scheduling analog31Swiss scheduling paper provides comparative EU/DACH legal context; NPS review provides broad legal framework
10Webproscaline PiHKAL Shulgin legal status controlled substance102Primary source for PiHKAL data on proscaline; confirmed legal status across jurisdictions
11PubMedNichols psychedelics SAR phenethylamine 5-HT2A mescaline21Authoritative SAR review covering mescaline class directly relevant to proscaline
12PubMedhallucinogen persisting perception disorder HPPD phenethylamine psychedelic21HPPD risk data for 5-HT2A agonist class; relevant to harm reduction section for proscaline
13PubMedpsychedelic cross tolerance 5-HT2A serotonin receptor downregulation11Mechanistic data on 5-HT2A tolerance directly relevant to proscaline's tolerance profile
14Erowidproscaline PiHKAL entry #14011Primary source for physical properties, dosage, effects, and synthesis of proscaline
15UK Legislationphenethylamine UK Misuse of Drugs Act Schedule 211Primary legal source confirming UK Class A status of proscaline via generic phenethylamine clause
16Webproscaline Australia Canada legal status101Jurisdictional coverage needed for legal status section
17MultipleProscaline dose data verification - DB vs PiHKAL vs PsychonautWiki31Cross-reference confirmed dose data alignment across sources - no contradictions found
18Webproscaline CAS number 39201-78-0 SMILES InChI103Chemical identity data confirmed from multiple independent registry sources
19PubMedphenethylamine 5-HT2B receptor cardiac valvulopathy serotonin agonist risk11Cardiac risk context for phenethylamine class
20UK Legislationphenethylamine MDA 1971 Schedule 2 generic clause11Primary source confirming UK legal status
41 claims by section — every cited sentence, checked against its source
safety10 · 5 ok
  • Claim in safety — inconclusiveinconclusiveworking →

  • Nausea and emesis are common dose-dependent adverse effects of mescaline, occurring frequently at 800 mg oralsupported

    Nausea/emesis at 800mg. s41398-024-03116-2

  • Hallucinogen Persisting Perception Disorder (HPPD) — persistent visual disturbances following psychedelic use — is documented for the 5-HT₂A agonist class, with case reports involving potent full agonists such as 25I-NBOMesupported

    5-HT2A receptor agonists pose risks of acute intoxication and long-term effects including hallucinogen persisting perception disorder (HPPD), derealization, and depersonalization. j.biopha.2021.112295

  • Tolerance to proscaline's effects develops rapidly through 5-HT₂A receptor density downregulation in frontal cortex, a mechanism demonstrated for the 5-HT₂A agonist class using DOI as a probe compoundsupported

    DOI repeated administration induces progressive tolerance to HTR via 5-HT2A downregulation. acschemneuro.2c00170

  • Full cross-tolerance exists among 5-HT₂A agonist psychedelics, including lsd, psilocybin, mescaline, dmt, and the DOx seriespartially supported

    Cross-tolerance between DOI and LSD. Nonpsychedelic 5-HT2A agonist lisuride did not produce cross-tolerance. acschemneuro.2c00170

  • Claim in safety — not_supportednot supportedworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • 5-HT₂A antagonists (ketanserin, haloperidol, risperidone, clozapine) attenuate or block the psychedelic effects of mescaline-class compounds, confirmed in controlled human studies.partially supported

    5-HT2A mediation confirmed via ketanserin. s41398-024-03116-2

  • Claim in safety — inconclusiveinconclusiveworking →

pharmacology7 · 5 ok
  • The mouse head-twitch response (HTR) — a behavioral readout mediated exclusively by 5-HT₂A activation and abolished by selective antagonists such as ketanserin and M100907 — is reliably elicited by proscalinesupported

    HTR dose-response experiments with mescaline, escaline and proscaline in C57BL/6J mice. 0269881119826610

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • For the 3,4,5-substituted phenethylamine series, conformational mobility of the 3- and 5-methoxy groups is required for receptor activation, as demonstrated by conformationally restricted analogs that lose activity when ring rotation is preventedsupported

    3,4,5-trioxygenated analogs require conformationally mobile 3 and 5 methoxy groups. pmid:9301661

  • In a randomized, double-blind, placebo-controlled crossover study (n = 16), oral mescaline showed dose-proportional pharmacokinetics across 100–800 mg, with a Tmax of approximately 2 hours, a plasma elimination half-life of approximately 3.5 hours, and subjective effect durations of 6.4–14 hours (dose-dependent).supported

    RCT in 16 subjects. Mescaline 100-800mg. Tmax ~2h, plasma half-life ~3.5h. Duration 6.4-14h dose-dependent. s41398-024-03116-2

  • Mescaline undergoes three principal metabolic transformations:supported

    LC-MS/MS method for mescaline and metabolites TMPAA, NAM, 4-desmethyl mescaline in human plasma. j.jpba.2022.114980

  • Mescaline undergoes three principal metabolic transformations:supported

    Review of mescaline PK/PD, mechanism of action, metabolism, duration, clinical and forensic aspects. 1874467211666181010154139

receptor-pharmacology6 · 5 ok
  • Proscaline's psychedelic activity is mediated by 5-HT₂A agonism, confirmed behaviorally through the HTR assaysupported

    HTR dose-response experiments with mescaline, escaline and proscaline in C57BL/6J mice. Potency relationships closely parallel human hallucinogenic data. 0269881119826610

  • The α-methyl analog 3C-P demonstrates higher intrinsic activity at 5-HT₂A-coupled phospholipase C signaling relative to the parent phenethylamine proscaline, consistent with the general finding that α-methylation increases functional efficacy at this receptor.supported

    Alpha-methylation increases intrinsic activity significantly. pmid:16277614

  • Homology modeling and SAR studies of the mescaline class indicate that conformational freedom of the 3- and 5-methoxy substituents is required for productive binding at the 5-HT₂A orthosteric sitesupported

    3,4,5-trioxygenated analogs require conformationally mobile 3 and 5 methoxy groups. pmid:9301661

  • Claim in receptor-pharmacology — not_supportednot supportedworking →

  • Proscaline retains this conformational mobility; its enhanced potency relative to mescaline in the HTR assay is attributed to the increased lipophilicity and steric properties of the 4-propoxy group.supported

    Replacing 4-methoxy with ethoxy or propoxy increases potency. 0269881119826610

  • Sustained 5-HT₂B agonism is associated with cardiac valvulopathy, as documented with fenfluramine and related compoundssupported

    5-HT hypothesis for fenfluramine-induced valvular heart disease. 5-HT2B receptor agonism linked to cardiac risk. 14740330902931524

comparative-pharmacology5 · 3 ok
  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Halberstadt et al. (2019) established the relative potency order of 3,4,5-substituted phenethylamines in the mouse HTR assay: proscaline (4-propoxy) > escaline (4-ethoxy) > mescaline (4-methoxy)supported

    HTR dose-response experiments with mescaline, escaline and proscaline in C57BL/6J mice. Replacing 4-methoxy with ethoxy or propoxy increases potency. 0269881119826610

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • The translational validity of mouse HTR data for predicting human hallucinogenic potency is supported by a strong correlation (r = 0.9448) across 41 compoundssupported

    Strong positive correlation r=0.9448 between mouse HTR and human hallucinogenic potency. Supports translational relevance of HTR assay. j.neuropharm.2019.107933

  • The α-methyl analog of proscaline (3C-P) shows higher intrinsic activity at 5-HT₂A-coupled phospholipase C activation. α-Methylation generally increases oral bioavailability (through resistance to MAO-mediated first-pass deamination), duration of action, and functional efficacy at 5-HT₂Apartially supported

    Alpha-methylation increases intrinsic activity significantly. pmid:16277614

summary5 · 4 ok
  • Active at oral doses of 30–60 mg, it produces effects lasting 8–12 hours — comparable to mescaline in duration but substantially greater in potency per milligram, as confirmed in the mouse head-twitch response (HTR) assay.partially supported

    HTR dose-response experiments with mescaline, escaline and proscaline in C57BL/6J mice. Replacing 4-methoxy with ethoxy or propoxy increases potency. 0269881119826610

  • A single peer-reviewed behavioral study confirmed increased HTR potency relative to mescaline in micesupported

    HTR dose-response experiments with mescaline, escaline and proscaline in C57BL/6J mice. Replacing 4-methoxy with ethoxy or propoxy increases potency. 0269881119826610

  • As a 3,4,5-trisubstituted phenethylamine, proscaline is presumed to act primarily through 5-HT₂A receptor agonism — the established mechanism for psychedelic effects in this structural classsupported

    Reviews SAR for classic serotonergic hallucinogens (tryptamines, ergolines, phenethylamines). 5-HT2A as principal target. Key structural features for activity discussed including the 3,4,5-trimethoxyphenethylamine (mescaline) class. 7854_2017_475

  • Tolerance develops rapidly through 5-HT₂A receptor downregulation in frontal cortex, with full cross-tolerance to other serotonergic psychedelics; the compound is not considered habit-formingsupported

    DOI repeated administration induces progressive tolerance to HTR via 5-HT2A downregulation. Cross-tolerance between DOI and LSD. acschemneuro.2c00170

  • Claim in summary — inconclusiveinconclusiveworking →

pharmacokinetic-detail4 · 4 ok
  • Mescaline is well absorbed orally, with dose-proportional kinetics across the 100–800 mg range and a Tmax of approximately 2 hourssupported

    Mescaline 100-800mg. Tmax ~2h. s41398-024-03116-2

  • Mescaline's three major metabolic routes — N-acetylation, O-demethylation, and MAO-A-mediated oxidative deamination — are documented analyticallysupported

    LC-MS/MS method for mescaline and metabolites TMPAA, NAM, 4-desmethyl mescaline in human plasma. j.jpba.2022.114980

  • Mescaline's three major metabolic routes — N-acetylation, O-demethylation, and MAO-A-mediated oxidative deamination — are documented analyticallysupported

    Review of mescaline PK/PD, mechanism of action, metabolism, duration, clinical and forensic aspects. 1874467211666181010154139

  • Mescaline's plasma elimination half-life is approximately 3.5 hours, yet subjective effects persist 6.4–14 hours (dose-dependent)supported

    Plasma half-life ~3.5h. Duration 6.4-14h dose-dependent. s41398-024-03116-2

chemistry1 · 1 ok
  • The α-methyl (amphetamine) homologue of proscaline is 3C-P, which shares the same ring substitution pattern but incorporates an additional methyl group on the side chain α-carbon, conferring increased intrinsic activity at 5-HT₂A-mediated phospholipase C signaling.supported

    Alpha-methylation increases intrinsic activity significantly. pmid:16277614

history1 · 1 ok
  • The sole formal pharmacological study — Halberstadt et al. (2019) — measured proscaline's behavioral potency in mice as part of a broader structure-activity relationship investigation of mescaline analogs, confirming greater HTR potency than both mescaline and escaline.supported

    HTR dose-response experiments with mescaline, escaline and proscaline in C57BL/6J mice. Replacing 4-methoxy with ethoxy or propoxy increases potency. 0269881119826610

legal-status1 · 1 ok
  • Proscaline's direct structural derivation from mescaline — differing only in the 4-position alkoxy group — and its confirmed 5-HT₂A agonist activity would likely satisfy both criteriasupported

    HTR dose-response experiments with mescaline, escaline and proscaline in C57BL/6J mice. Potency relationships closely parallel human hallucinogenic data. 0269881119826610

neuroscience1 · 0 ok
  • Claim in neuroscience — inconclusiveinconclusiveworking →

3Sources

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

Sources
yearsourcetierstatusfeeds
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/s41398-024-03116-2strongconsumed5 sections
2024NCATS Inxight Drugs — Proscaline (GSRS record 99G781N5IO)NIH National Center for Advancing Translational Sciencesurl:c871444a9ac5ae75weakconsumedcited only
2024Oxycodone legal status - UK Class A/CD2, Australia Schedule 8, Canada Schedule I, US Schedule IIVarious government sourcesurl:8e889d7d8596ec6cweakconsumedcited only
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
2022Development and validation of an LC-MS/MS method for the quantification of mescaline and major metabolites in human plasmaThomann J, Ley L, Klaiber A, Liechti ME, Duthaler U · Journal of Pharmaceutical and Biomedical Analysisdoi:10.1016/j.jpba.2022.114980moderateconsumed3 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
2020Correlation between the potency of hallucinogens in the mouse head-twitch response assay and their behavioral and subjective effects in other speciesHalberstadt AL, Chatha M, Klein AK, Wallach J, Brandt SD · Neuropharmacologydoi:10.1016/j.neuropharm.2019.107933moderateconsumed3 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:10.1177/0269881119826610moderateconsumed6 sections
2019Pharmacokinetic and Pharmacodynamic Aspects of Peyote and Mescaline: Clinical and Forensic RepercussionsDinis-Oliveira RJ, Pereira CL, da Silva DD · Current Molecular Pharmacologydoi:10.2174/1874467211666181010154139moderateconsumed3 sections
2018Chemistry and Structure-Activity Relationships of Psychedelics.Nichols DE · Current Topics in Behavioral Neurosciencesdoi:10.1007/7854_2017_475strongconsumed3 sections
2009Serotonergic drugs and valvular heart diseaseRothman RB, Baumann MH · Expert Opinion on Drug Safetydoi:10.1517/14740330902931524moderateconsumed1 section
2006C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptorMcLean TH, Chambers JJ, Parrish JC, Braden MR, Marona-Lewicka D, Kurrasch-Orbaugh D, Nichols DE · Journal of Medicinal Chemistrypmid:16821786moderateconsumed1 section
2005Differential phospholipase C activation by phenylalkylamine serotonin 5-HT2A receptor agonistsParrish JC, Braden MR, Gundy E, Nichols DE · Journal of Neurochemistrypmid:16277614moderateconsumed3 sections
1997Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivativesMonte AP, Waldman SR, Marona-Lewicka D, Wainscott DB, Nelson DL, Sanders-Bush E, Nichols DE · Journal of Medicinal Chemistrypmid:9301661moderateconsumed2 sections
1991PiHKAL Entry #140: Proscaline (3,5-dimethoxy-4-(n)-propoxyphenethylamine)Shulgin ATurl:afc560a8ac3f7b84weakconsumedcited only
—Searched ClinicalTrials.gov for "proscaline" — no resultsabsenceno results—
—Searched ClinicalTrials.gov for "proscaline" — no resultsabsenceno results—

4Docket

one filing per activity — decisions, correspondence, reports

  1. 0012026-05-03revisionRevision 1

    Initial LLM generation (v5 pipeline, wiki)

    psx:substance/proscaline/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

    • 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 · cardiovascular
    • contraindication · other
    • contraindication · other
    • contraindication · pregnancy_breastfeeding
    psx:substance/proscaline/proposal/dose_tier/263ce2dc-2e30-401e-8674-15fee44c8c0e
  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 20:33Revision 1current
info_card2e08aea07032cbfea4537490…2026-10-19 20:33Revision 1current
noticef069a9dea47b308467344618…2026-10-19 20:33Revision 1current
emergency3f0909c25c714d225b4bb3e3…2026-09-04 04:32Revision 1superseded2026-10-19
info_cardb63c1e2eda9fa89dbaed7ce6…2026-09-04 04:32Revision 1superseded2026-10-19
notice64878b43a1d2932a5305f55b…2026-09-04 04:32Revision 1superseded2026-10-19