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psx:substance/isopropylphenidate/src/doi:10.1007/s40263-013-0084-8

src2026-09-24recordconsumed

derived from · upstream

none recorded

feeds · downstream

Closure of psx:substance/isopropylphenidate/src/doi:10.1007/s40263-013-0084-8: 45 upstream, 76 downstream.

psx:substance/isopropylphenidate/src/doi:10.1007/s40263-013-0084-8
  ├─ used  src/doi:10.1089/cap.2013.0074  Isopropylphenidate: an ester homolog of methylphenidate with sustained and selective dopaminergic activity and reduced drug interaction liability
  ├─ used  src/url:783650e749d86b22  US Patent US20120245201A1: Isopropylphenidate for Treatment of ADHD and Fatigue-Related Disorders
  ├─ used  src/doi:10.26355/eurrev_201901_16741  Use of cognitive enhancers: methylphenidate and analogs
  ├─ used  src/doi:10.1007/s00204-020-02693-7  Designer drugs: mechanism of action and adverse effects
  ├─ used  src/doi:10.1016/j.drugpo.2023.104109  No prescription? No problem: A qualitative study investigating self-medication with novel psychoactive substances (NPS)
  ├─ used  src/url:ec0798ba86d0bb86  UK Temporary Class Drug Order: Methylphenidate-based NPS (ACMD Report, April 2015)
  ├─ used  src/url:cd066895e93f8534  UNODC Early Warning Advisory: UK temporarily bans five methylphenidate-related NPS (April 2015)
  ├─ used  src/url:2c09a455e415ab0a  Germany NpSG: New Psychoactive Substances Act (Neue-psychoaktive-Stoffe-Gesetz) November 2016
  ├─ used  src/url:e65534339fe76a9f  Canada Gazette: Amendments to Controlled Drugs and Substances Act Schedule III (methylphenidate analogues)
  ├─ used  src/url:249e0f66de3cb475  UK control of methylphenidate-based NPS: Misuse of Drugs (Amendment) Regulations 2017
  ├─ used  src/pmid:17228864  Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter
  ├─ used  src/doi:10.1002/dta.2161  Analysis of six 'neuro-enhancing' phenidate analogs
  ├─ used  src/doi:10.1016/j.neuropharm.2017.08.020  Pharmacological profile of methylphenidate-based designer drugs
  ├─ used  src/doi:10.4414/smw.2015.14043  Novel psychoactive substances (designer drugs): overview and pharmacology of modulators of monoamine signaling
  ├─ used  src/doi:10.1124/dmd.112.048595  Differential influences of ethanol on early exposure to racemic methylphenidate compared with dexmethylphenidate in humans
  ├─ used  src/doi:10.1093/jat/bkz052  Use of UPLC-HRMS/MS for In Vitro and In Vivo Metabolite Identification of Three Methylphenidate-derived New Psychoactive Substances
  ├─ used  src/doi:10.1016/j.jpba.2015.09.029  Identification of in vitro metabolites of ethylphenidate by liquid chromatography coupled to quadrupole time-of-flight mass spectrometry
  ├─ used  src/doi:10.3389/fpsyt.2020.546796  The Psychonauts' World of Cognitive Enhancers
  ├─ used  src/doi:10.1002/jps.24202  Ethylphenidate as a selective dopaminergic agonist and methylphenidate-ethanol transesterification biomarker.
  ├─ used  src/doi:10.1016/j.forsciint.2015.12.045  Seven fatalities associated with ethylphenidate.
  ├─ used  src/doi:10.1080/17512433.2023.2279192  Stimulant and hallucinogenic novel psychoactive substances; an update
  ├─ used  src/pmid:8332631  A comparison of the motor-activating effects of acute and chronic exposure to amphetamine and methylphenidate
  ├─ used  src/pmid:19724727  Tramadol: seizures, serotonin syndrome, and coadministered antidepressants
  ├─ used  src/doi:10.1016/j.amjmed.2018.04.025  Tramadol: Understanding the Risk of Serotonin Syndrome and Seizures
  ├─ used  src/doi:10.1017/S1461145713001132
  ├─ used  src/doi:10.1039/d5cs01021g  Nemo censetur ignorare legem: what research chemists should know about the EU legal framework
  ├─ derived_from  gen/1406d612-8b77-4695-bc24-972260bf9644  Generation — pipeline-v5
  ├─ generated_by  pub/1d4be182-26dc-40b1-8ada-c541bbf46135  Publication — backfill
    ├─ used  search/da982329-9164-40f4-8391-2b2a2797422a  Searched PubChem for "isopropylphenidate"
    ├─ used  search/7fa0eb56-6ae4-4ab0-a6da-490a67783c69  Searched PubMed for "isopropylphenidate pharmacology"
    ├─ used  search/96a61206-4419-4984-b67b-ad4093765ae4  Searched PubMed for "isopropylphenidate IPH stimulant"
    ├─ used  search/93a4fb01-7534-43cb-ac46-e648d92376a8  Searched ClinicalTrials.gov for "isopropylphenidate"
    ├─ used  search/478fafcc-3aa3-4547-bf5a-fbf19344e0b3  Searched PubMed for "methylphenidate carboxylesterase hydrolysis ethanol transesterification"
    ├─ used  search/9da8ce51-7bf9-4010-8870-9acfcabe0e2e  Searched OpenAlex for "isopropylphenidate pharmacology dopamine"
    ├─ used  search/7332e1ea-e379-4d35-a85f-96ffbf53d2fc  Searched OpenAlex for "methylphenidate phenidate new psychoactive substances forensic detection"
    ├─ used  search/d0d0a627-3e7e-40dc-bf1f-ef715b5019e0  Searched WebSearch for "isopropylphenidate legal status scheduling UK US EU Australia 2024"
    ├─ used  search/4eb0c1d5-a3a5-4af1-a1cd-05aca2be8b91  Searched WebSearch for "isopropylphenidate Canada Schedule III controlled drugs substances"
    ├─ used  search/ade770cf-8cda-4808-bf65-0537a9e7ee3c  Searched WebSearch (via Grokipedia) for "isopropylphenidate pharmacological data"
    ├─ used  search/3259ece6-49b3-4ab6-96a0-3f7c199e4387  Searched PubMed/Crossref DOI verification for "DOI 10.1089/cap.2013.0074"
    ├─ used  search/e91de2f7-0084-49f9-b36a-599834c67939  Searched PubMed for "methylphenidate MDMA co-administration interaction serotonin cardiovascular"
    ├─ used  search/cd58193f-b9b5-4dcb-8d30-fdc5fb446ded  Searched PubMed for "methylphenidate adverse effects cardiovascular hypertension clinical review"
    ├─ used  search/6c46d6d9-7e0c-4993-9156-a68eebd8b394  Searched WebSearch for "stimulant tramadol dangerous interaction seizure serotonin"
    ├─ used  search/b3e95837-f83c-4cd1-968f-457169d4d205  Searched Multiple sources for "Verification of chemical data against PubChem and secondary sources"
    ├─ used  search/4081546e-7735-4e7a-96f7-a1f94ac29222  Searched Grokipedia (web_retrieved) for "isopropylphenidate binding affinity specific values"
    └─ used  search/2bc8e073-27c4-4ce8-bda3-59ba413815fb  Searched WebSearch for "isopropylphenidate legal status UK US Germany Canada Australia"
├─ used  version/1  Revision 1
├─ used  claim/89acfd2e-f002-448d-8863-7318260ec7ed  Claim in summary — partially_supported
├─ used  claim/d5de7392-1569-425b-b29a-43834cccb049  Claim in safety — supported
├─ used  claim/21de8cd5-4323-415b-8da8-a982a3d818c7  Claim in safety — supported
  ├─ derived_from  issue/notice@dc91d6955c9b  Issued notice
  ├─ derived_from  issue/info_card@ff3ab5c76728  Issued info_card
  ├─ derived_from  issue/emergency@58d3299a8754  Issued emergency
  ├─ derived_from  issue/info_card@ab5c50b066ea  Issued info_card
  ├─ informed_by  section/summary.full@1
  ├─ informed_by  section/safety.full@1
    ├─ used  claim/3ff86ebd-c527-4916-a2ee-075c39169e97  Claim in summary — inconclusive  working
    ├─ used  claim/0625cc5f-a75e-4eee-b29d-ca1dc7bf1936  Claim in summary — inconclusive  working
    ├─ used  claim/31af06ed-35fb-496c-9a9a-e8d0aa2a88e4  Claim in summary — inconclusive  working
    ├─ used  claim/09ff95ae-c656-4518-aa82-710b3fcce9d9  Claim in pharmacology — inconclusive  working
    ├─ used  claim/0dc45abd-9ec0-4e0a-8661-d447a85e913c  Claim in pharmacology — inconclusive  working
    ├─ used  claim/61111dd0-5620-4819-a9b5-3fa87611cf1c  Claim in pharmacology — supported
    ├─ used  claim/dbb7a1c9-b6aa-4f7d-8047-8c543f6bdde5  Claim in pharmacology — inconclusive  working
    ├─ used  claim/71b271c8-26a6-4727-9bc0-13a61d784679  Claim in pharmacology — supported
    ├─ used  claim/44e3d88a-1dcf-4301-af3c-5b7faefe912e  Claim in clinical-evidence — inconclusive  working
    ├─ used  claim/9082f671-eccc-4484-83cf-aef7e0fdc535  Claim in clinical-evidence — inconclusive  working
    ├─ used  claim/675c5ca2-bb7d-41e2-ab75-5d674018f4d1  Claim in safety — supported
    ├─ used  claim/93b5768d-064d-4b1c-a225-34b2738e340d  Claim in safety — supported
    ├─ used  claim/30e8c5c4-81a4-4e59-a7c6-4f0e808a49a3  Claim in history — inconclusive  working
    ├─ used  claim/f6df8974-2123-4c75-975b-fb9ce931707f  Claim in chemistry — supported
    ├─ used  claim/e5938864-96b8-44b0-a7e7-75c3eb5fa341  Claim in chemistry — supported
    ├─ used  claim/88054126-c5c9-432b-917c-8ef16c19459e  Claim in receptor-pharmacology — supported
    ├─ used  claim/f51dc9f2-9c6b-43c8-a735-9d13aa1d3d98  Claim in receptor-pharmacology — supported
    ├─ used  claim/bde384e5-e73e-412e-8741-dac3535c3202  Claim in receptor-pharmacology — inconclusive  working
    ├─ used  claim/9bdb043f-0ff2-4480-9841-7805616d5785  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/0201fd01-5115-40dd-9a58-f53930683fa7  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/a1ef1e21-c92d-4a02-bc0d-bb4084981db5  Claim in history — inconclusive  working
    ├─ used  claim/9ca192db-a778-4abd-b094-e2652cdcffc8  Claim in history — inconclusive  working
    ├─ used  claim/862804ca-c73f-42d7-a6a2-627f0fbd6d9d  Claim in comparative-pharmacology — supported
    ├─ used  claim/abf39c6b-e389-49d7-ad15-e79fd2b71e97  Claim in safety — inconclusive  working
    ├─ used  claim/97285aa3-1de4-45d5-be98-7e7dd70be24f  Claim in history — supported
    ├─ used  claim/dc3c8284-4d28-4701-91d3-548e6981b48a  Claim in clinical-evidence — supported
    ├─ used  claim/371ff864-0c4d-4e57-b1b4-dc5fd5554eb5  Claim in chemistry — supported
    ├─ used  claim/e0076e99-2d3c-4d39-bc4f-e6f2d5938cc5  Claim in chemistry — supported
    ├─ used  claim/03dd04c8-59b6-44b3-a456-0ea15df9526a  Claim in chemistry — inconclusive  working
    ├─ used  claim/6300deb0-4471-4f15-aef7-d5796b307a6c  Claim in chemistry — supported
    ├─ used  claim/f1d33981-968b-4089-8ebd-4a5a84444cc8  Claim in pharmacology — inconclusive  working
    ├─ used  claim/f0532dd3-08c7-467a-a4ed-5015389b4f5d  Claim in receptor-pharmacology — supported
    ├─ used  claim/6d87d0cf-41fe-4448-9a1f-6d7ea58c5796  Claim in pharmacology — inconclusive  working
    ├─ used  claim/8b2537ee-70ba-454b-93ed-521b6d73839a  Claim in receptor-pharmacology — inconclusive  working
    ├─ used  claim/aa11a665-0d16-43d9-895c-521df3e79c52  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/0a648caf-c2aa-4ff7-9b9b-06babafeafba  Claim in pharmacology — supported
    ├─ used  claim/b067293c-66b5-4f29-84cd-a7329e555466  Claim in pharmacology — inconclusive  working
    ├─ used  claim/722c8d8d-5f9b-4f33-a6da-57ede1eac7e3  Claim in safety — supported
    ├─ used  claim/15c0638f-f3a9-46ea-946c-74835672f40c  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/5afd108a-e401-4941-b385-ba5d973cb205  Claim in pharmacology — supported
    ├─ used  claim/1be470c8-1853-41be-9598-94071f4cabf7  Claim in pharmacology — inconclusive  working
    ├─ used  claim/bc3f4f28-a43f-4c63-9c69-1aad0315e5d5  Claim in pharmacology — supported
    ├─ used  claim/300461ec-2fb4-4068-9f94-82aa886d2c1d  Claim in pharmacokinetic-detail — supported
    ├─ used  claim/0919402c-ff93-49e1-987e-4f6df9d67696  Claim in clinical-evidence — supported
    ├─ used  claim/d95d2afb-ef0d-4373-b127-0078fbfe098f  Claim in pharmacology — supported
    ├─ used  claim/f3a9d097-ce85-46db-8bfb-df5c32269d1f  Claim in pharmacokinetic-detail — supported
    ├─ used  claim/3ea7426d-35ae-46ab-8691-9823acb5747a  Claim in clinical-evidence — supported
    ├─ used  claim/9a822675-7729-46be-a2a8-41ef8012ca1e  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/c16388ec-20be-447f-8ced-a99413f2e8ec  Claim in comparative-pharmacology — supported
    ├─ used  claim/d8b7e43b-a0d5-47d5-94b8-700aff3d725b  Claim in comparative-pharmacology — supported
    ├─ used  claim/638783de-a920-4a92-9d3a-cd37fcca9b96  Claim in safety — supported
    ├─ used  claim/dbdc3bf8-1b54-445d-a8d3-006994db9333  Claim in comparative-pharmacology — inconclusive  working
    ├─ used  claim/30fef32c-2aee-48d3-a982-03a6d97a50b4  Claim in safety — supported
    ├─ used  claim/3e863ab8-d992-442f-bcdc-edbdf6f4a4f3  Claim in neuroscience — supported
    ├─ used  claim/cc319d51-8c35-401c-ae26-25a270ad781e  Claim in neuroscience — supported
    ├─ used  claim/e4bad31f-4dcb-4225-afc7-de781e6485e1  Claim in safety — supported
    ├─ used  claim/516ba6b7-4b1c-473c-aefc-3f7531f93838  Claim in safety — supported
    ├─ used  claim/01b5162e-5b1a-41d7-9e10-dacc9d229306  Claim in safety — supported
      ├─ informed_by  section/pharmacology.full@1
      ├─ informed_by  section/clinical-evidence.full@1
      ├─ informed_by  section/history.full@1
      ├─ informed_by  section/chemistry.full@1
      ├─ informed_by  section/receptor-pharmacology.full@1
      ├─ informed_by  section/comparative-pharmacology.full@1
      ├─ informed_by  section/pharmacokinetic-detail.full@1
      └─ informed_by  section/neuroscience.full@1

indented by distance from this node, not by parentage

1Provenance card

the boundary, as counts

Sources

2718 with DOI

2 strong · 18 moderate · 7 weak

Compilations

12026-05-11T23:24:11.950Z

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

Decisions

43last ruled 2026-06-04

0 awaiting a ruling

Issued documents

42026-10-19T20:32:21.117Z

notice · info card · emergency

Searches

171 with no results

queries and counts on the build

Claims checked

6136 supported

36 supported · 25 not

Correspondence

0received

consent field ships in Phase 4

Edges

222

derivations recorded for this entity

Complete over 27 sources, 1 compilation, and 43 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/isopropylphenidate/archive

2Build

one panel per compilation run

generation run 2026-05-11

58 min completedmodel pipeline-v5plan not recordedrun/217f1079…

Selection

results seen91
selected by the model39
consumed as sources27

Verification

claims checked61
supported35
partially supported1
not supported0
inconclusive25
  • record
  • seen / partial
  • working

The model's own caveats

  • sparse_evidence
  • structural_inference

Reproduce

inputs
27 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
17 searches — query, source, results, what was kept and why
17 searches for this run
#sourcequeryseenkeptrationale
1PubMedisopropylphenidate pharmacology54All directly relevant to IPH pharmacology and toxicology
2ClinicalTrials.gov · absenceisopropylphenidate00No trials exist; gap to note in output
3PubMedisopropylphenidate IPH stimulant22Already captured; no new results
4PubChemisopropylphenidate11Primary chemical identity data for isopropylphenidate
5PubMedmethylphenidate carboxylesterase hydrolysis ethanol transesterification21Relevant to IPH's reduced CES1 interaction advantage
6OpenAlexmethylphenidate phenidate new psychoactive substances forensic detection104Phenidate class forensic characterization, safety context, and comparative pharmacology
7OpenAlexisopropylphenidate pharmacology dopamine104Provide NPS class context and adverse effect profiles for phenidates
8PubMed/Crossref DOI verificationDOI 10.1089/cap.2013.007411Verification of primary pharmacology paper
9WebSearchisopropylphenidate Canada Schedule III controlled drugs substances101Canada scheduling confirmed
10WebSearch (via Grokipedia)isopropylphenidate pharmacological data13Specific binding data sourced from Markowitz 2013 paper - web retrieval only, cannot access full text directly
11WebSearchisopropylphenidate legal status scheduling UK US EU Australia 2024104Legal status data for major jurisdictions
12PubMedmethylphenidate MDMA co-administration interaction serotonin cardiovascular11Direct evidence for MPH-class+MDMA dangerous cardiovascular interaction
13WebSearchisopropylphenidate legal status UK US Germany Canada Australia203Legal status across major jurisdictions
14Grokipedia (web_retrieved)isopropylphenidate binding affinity specific values13Only available numerical binding data; flagged as requiring full-text verification
15WebSearchstimulant tramadol dangerous interaction seizure serotonin102Mechanism for tramadol 'lethal' interaction with IPH
16Multiple sourcesVerification of chemical data against PubChem and secondary sources33Chemical identity cross-verification
17PubMedmethylphenidate adverse effects cardiovascular hypertension clinical review42Overdose management and cardiovascular data directly applicable to IPH as MPH analog
61 claims by section — every cited sentence, checked against its source
pharmacology13 · 6 ok
  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • This resistance has two major consequences: sustained pharmacological action beyond methylphenidate's typical 2–3 hour effective window, and substantially reduced ethanol interaction via the CES1-mediated transesterification pathway that converts methylphenidate to ethylphenidate in the presence of alcohol.supported

    greater resistance to hydrolysis and transesterification via CES1 relative to MPH. Sustained psychostimulant properties in rats with locomotor activity as pharmacodynamic outcome. cap.2013.0074

  • This resistance has two major consequences: sustained pharmacological action beyond methylphenidate's typical 2–3 hour effective window, and substantially reduced ethanol interaction via the CES1-mediated transesterification pathway that converts methylphenidate to ethylphenidate in the presence of alcohol.supported

    CES1-mediated enantioselective hydrolysis and transesterification. Relevant to IPH's reduced CES1 hydrolysis and reduced ethanol interaction risk. dmd.112.048595

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Manier and colleagues identified 17 metabolites of IPH in rat urine using ultra-high-performance liquid chromatography–high-resolution tandem mass spectrometry (UHPLC-HRMS/MS): 14 phase I metabolites and 3 phase II metabolitessupported

    Identified 17 metabolites of IPH (14 phase I, 3 phase II) in rat urine using UHPLC-HRMS/MS. bkz052

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • Carboxy metabolites are recommended as analytical targets alongside the parent compound for toxicological screening.supported

    Carboxy metabolites recommended as additional analytical targets for comprehensive screening. bkz052

  • By analogy with ethylphenidate, the closest well-studied phenidate analog, CYP2C19 is likely the most active oxidative isoform, with contributions from CYP1A2, CYP2B6, CYP2C9, CYP2D6, and CYP3A4.supported

    CYP2C19 most active. rCYP1A2, 2B6, 2C9, 2D6, 3A4 also involved. j.jpba.2015.09.029

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • The duration data available (oral total 3.5–6 hours, insufflated total 2.5–4 hours) derive exclusively from user self-reports and are consistent with the animal data demonstrating sustained activity relative to methylphenidate.supported

    Sustained psychostimulant properties in rats with locomotor activity as pharmacodynamic outcome. cap.2013.0074

safety11 · 10 ok
  • The closely related ethylphenidate has been associated with 7 documented fatalities, establishing that phenidate-class analogs carry real toxicity risk despite the absence of IPH-specific fatality data.supported

    7 cases with ethylphenidate (EPH) detected in postmortem blood (Feb 2013-Jan 2015). All male, ages 23-49. One case sole EPH toxicity; 4 mixed drug toxicity; 2 hangings. j.forsciint.2015.12.045

  • Given IPH's mechanism as a DAT/NET reuptake inhibitor, its acute overdose toxicology is expected to parallel methylphenidate overdose presentations. Anticipated features include:supported

    MPH overdose features mydriasis, tremor, agitation, hyperreflexia, hallucinations, delirium, seizures. Mechanism: excessive DA/NE/5-HT. s40263-013-0084-8

  • {{Emergency}}In suspected isopropylphenidate overdose, management follows methylphenidate/stimulant overdose protocol: benzodiazepines as first-line treatment for agitation and seizures, supportive cardiovascular management, continuous temperature monitoring, and poison control consultation.{{/Emergency}}supported

    Management: benzodiazepines first-line; antipsychotics for refractory cases. s40263-013-0084-8

  • Tolerance to stimulant effects is expected with repeated administration, following the methylphenidate pattern of locomotor tolerance without behavioral sensitizationsupported

    Chronic MPH administration produces tolerance to locomotor activity (not sensitization like amphetamine). pmid:8332631

  • IPH's slower CES1 metabolism may confer somewhat reduced abuse liability compared to methylphenidate by reducing the rapid rise-and-fall plasma kinetics that drive reinforcement cyclessupported

    greater resistance to hydrolysis and transesterification via CES1 relative to MPH. Sustained psychostimulant properties in rats. cap.2013.0074

  • Claim in safety — inconclusiveinconclusiveworking →

  • Tramadol inhibits serotonin and norepinephrine reuptake (SNRI-like action) and significantly lowers the seizure thresholdsupported

    Tramadol inhibits serotonin and norepinephrine reuptake; seizures and serotonin syndrome are two significant adverse reactions. pmid:19724727

  • Tramadol inhibits serotonin and norepinephrine reuptake (SNRI-like action) and significantly lowers the seizure thresholdsupported

    Tramadol's SNRI activity underlies serotonin syndrome and seizure risks. j.amjmed.2018.04.025

  • A human randomized controlled trial demonstrated that methylphenidate (0.5 mg/kg) combined with MDMA (125 mg) produced significantly elevated cardiovascular adverse effects (heart rate, blood pressure) compared to either drug alone, without enhancement of desired subjective effectssupported

    MPH+MDMA in healthy subjects: combination does not increase psychoactive effects but significantly enhances cardiovascular and adverse effects compared to either alone. s1461145713001132

  • IPH's 10-fold CES1 resistance substantially reduces the transesterification pathway (methylphenidate + ethanol → ethylphenidate) that represents a pharmacokinetic drug interaction specific to methylphenidatesupported

    greater resistance to hydrolysis and transesterification via CES1 relative to MPH. cap.2013.0074

  • IPH's 10-fold CES1 resistance substantially reduces the transesterification pathway (methylphenidate + ethanol → ethylphenidate) that represents a pharmacokinetic drug interaction specific to methylphenidatesupported

    CES1-mediated enantioselective hydrolysis and transesterification. Relevant to IPH's reduced CES1 hydrolysis and reduced ethanol interaction risk. dmd.112.048595

comparative-pharmacology9 · 3 ok
  • EPH has been associated with 7 documented fatalities, while no fatalities have been attributed to IPHsupported

    7 cases with ethylphenidate (EPH) detected in postmortem blood (Feb 2013-Jan 2015). j.forsciint.2015.12.045

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Ethylphenidate (EPH) shares IPH's enhanced DAT selectivity but differs in metabolic stability and safety profile. d-EPH shows near-exclusive DAT action with minimal NET involvementsupported

    d-EPH selectively targets DAT; CES1 transesterification of MPH with ethanol. jps.24202

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Within the broader novel psychoactive stimulant landscape, IPH is notable for its relatively clean pharmacological profile (selective DAT inhibition without releasing activity, serotonergic effects, or off-target receptor binding), its sustained duration, and its reduced ethanol interaction liabilitysupported

    Stimulants including phenidate analogs interact primarily with monoamine transporters, causing sympathomimetic adverse effects. s00204-020-02693-7

chemistry6 · 5 ok
  • This single substitution increases steric bulk and lipophilicity at the ester position, conferring resistance to enzymatic hydrolysis by carboxylesterase-1 (CES1).supported

    greater resistance to hydrolysis and transesterification via CES1 relative to MPH. cap.2013.0074

  • Froimowitz and colleagues systematically explored alkyl ester modifications to the methylphenidate scaffold, establishing that increased ester chain length and branching generally enhances DAT selectivity and prolongs duration of action.supported

    MPH analogues with alkyl ester substitutions tested in monoamine transporter assays. Some show slow onset and long duration with enhanced DAT selectivity. pmid:17228864

  • Commercial and research samples of IPH are prepared exclusively in the threo configurationsupported

    Full characterization (X-ray, NMR, GC-MS, FTIR) of six phenidate analogs. Exclusive threo-configuration. dta.2161

  • The racemic threo mixture (dl-IPH) was used in the Markowitz 2013 characterizationsupported

    Investigated metabolic profiles and pharmacological activity of dl-isopropylphenidate (IPH) in vitro and in vivo. cap.2013.0074

  • Claim in chemistry — inconclusiveinconclusiveworking →

  • Phenidate analogs as a class exhibit thermal instability under gas chromatography–mass spectrometry (GC-MS) conditions, with decomposition occurring in the injection port; liquid chromatography–tandem mass spectrometry (LC-MS/MS) is therefore the preferred analytical method for forensic identification.supported

    Full characterization (X-ray, NMR, GC-MS, FTIR) of six phenidate analogs. Thermal decomposition in GC-MS. dta.2161

clinical-evidence5 · 3 ok
  • Claim in clinical-evidence — inconclusiveinconclusiveworking →

  • Claim in clinical-evidence — inconclusiveinconclusiveworking →

  • Manier and colleagues conducted in vitro metabolite identification using rat urine and human S9 fractions, establishing the metabolic profile for forensic and clinical analytical purposessupported

    Identified 17 metabolites of IPH (14 phase I, 3 phase II) in rat urine using UHPLC-HRMS/MS. Human S9 fraction indicated primary hydrolysis to carboxy metabolites. bkz052

  • In the absence of clinical evidence, isopropylphenidate has been adopted by individuals self-medicating for ADHD symptoms and cognitive enhancement, a pattern documented in qualitative research on novel psychoactive substance usesupported

    Subjects mainly self-treating ADHD, anxiety, depression. 4F-MPH (a phenidate) among most discussed. Motivations include access, cost, legality, dissatisfaction with healthcare. j.drugpo.2023.104109

  • In the absence of clinical evidence, isopropylphenidate has been adopted by individuals self-medicating for ADHD symptoms and cognitive enhancement, a pattern documented in qualitative research on novel psychoactive substance usesupported

    Growing availability of NPS as cognitive enhancers. Internet/psychonaut-reported use patterns. Identifies phenidate analogs among commonly reported cognitive enhancers. fpsyt.2020.546796

receptor-pharmacology5 · 3 ok
  • The primary pharmacological characterization of isopropylphenidate derives from Markowitz and colleagues, who assessed monoamine transporter inhibition using rat synaptosome and HEK293 transfected cell assays.supported

    Investigated metabolic profiles and pharmacological activity of dl-isopropylphenidate (IPH) in vitro and in vivo. cap.2013.0074

  • Markowitz and colleagues concluded that IPH exhibits "greater DAT than NET binding and cellular uptake activity," qualitatively confirming selective dopaminergic action over noradrenergic. The specific IC₅₀ values (DAT ~200 nM, NET >10,000 nM) are aggregated from secondary sources citing Markowitz 2013; full-text verification of these exact numerical values is required.supported

    IPH displayed greater DAT than NET binding and cellular uptake activity. cap.2013.0074

  • Luethi and colleagues characterized the pharmacological profile of IPH and related methylphenidate-based designer drugs in vitro using HEK293 cells transfected with human DAT, NET, and SERTsupported

    In vitro pharmacological characterization of methylphenidate-based NPS including IPH. Characterizes DAT/NET/SERT binding and uptake inhibition. j.neuropharm.2017.08.020

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

history4 · 1 ok
  • Claim in history — inconclusiveinconclusiveworking →

  • Claim in history — inconclusiveinconclusiveworking →

  • Claim in history — inconclusiveinconclusiveworking →

  • The compound was adopted primarily by individuals seeking cognitive enhancement or self-medicating for ADHD symptoms.supported

    Subjects mainly self-treating ADHD, anxiety, depression. 4F-MPH (a phenidate) among most discussed. Motivations include access, cost, legality, dissatisfaction with healthcare. j.drugpo.2023.104109

summary4 · 1 ok
  • Claim in summary — inconclusiveinconclusiveworking →

  • Claim in summary — inconclusiveinconclusiveworking →

  • Claim in summary — inconclusiveinconclusiveworking →

  • As a DAT/NET reuptake inhibitor, cardiovascular toxicity (tachycardia, hypertension) represents the primary acute risk at supratherapeutic doses, following the methylphenidate overdose profilepartially supported

    MPH overdose features mydriasis, tremor, agitation, hyperreflexia, hallucinations, delirium, seizures. Mechanism: excessive DA/NE/5-HT. s40263-013-0084-8

neuroscience2 · 2 ok
  • Chronic methylphenidate administration in rodents produces tolerance to locomotor effects rather than sensitization — a pattern that distinguishes phenidates from amphetamines, which characteristically produce behavioral sensitization with repeated dosingsupported

    Chronic MPH administration produces tolerance to locomotor activity (not sensitization like amphetamine). Suggests different mechanisms of tolerance development between reuptake blockers and releasers. pmid:8332631

  • Is the tolerance profile (tolerance without sensitization) confirmed in primates or humans? The rat data from McNamara 1993 apply to methylphenidate; IPH-specific tolerance neuroadaptation is unstudied.supported

    Chronic MPH administration produces tolerance to locomotor activity (not sensitization like amphetamine). Suggests different mechanisms of tolerance development between reuptake blockers and releasers. pmid:8332631

pharmacokinetic-detail2 · 2 ok
  • Structural analog inference from ethylphenidate suggests CYP2C19 as the primary oxidative isoform, with secondary contributions from CYP1A2, CYP2B6, CYP2C9, CYP2D6, and CYP3A4. Individuals who are CYP2C19 poor metabolizers may experience prolonged effects if this isoform is relevant to IPH oxidative metabolism, but this has not been studied.supported

    CYP2C19 most active. rCYP1A2, 2B6, 2C9, 2D6, 3A4 also involved. j.jpba.2015.09.029

  • CYP-mediated drug interactions are likely less clinically significant given that oxidative metabolism appears to be a secondary pathwaysupported

    Human S9 fraction indicated primary hydrolysis to carboxy metabolites. bkz052

3Sources

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

Sources
yearsourcetierstatusfeeds
2025Nemo censetur ignorare legem: what research chemists should know about the EU legal frameworkBianchi S, Campalani C, Vella V, Michel Q, Monbaliu J-CM · Chemical Society Reviewsdoi:10.1039/d5cs01021gmoderateconsumedcited only
2023No prescription? No problem: A qualitative study investigating self-medication with novel psychoactive substances (NPS)Holborn T, Schifano F, Deluca P · The International Journal on Drug Policydoi:10.1016/j.drugpo.2023.104109moderateconsumed3 sections
2023Stimulant and hallucinogenic novel psychoactive substances; an updateSchifano F, Vento A, Scherbaum N, Guirguis A · Expert Review of Clinical Pharmacologydoi:10.1080/17512433.2023.2279192moderateconsumed1 section
2020Designer drugs: mechanism of action and adverse effectsLuethi D, Liechti ME · Archives of Toxicologydoi:10.1007/s00204-020-02693-7strongconsumed2 sections
2020The Psychonauts' World of Cognitive EnhancersNapoletano F, Schifano F, Corkery JM, Guirguis A, Arillotta D, Zangani C, Vento A · Frontiers in Psychiatrydoi:10.3389/fpsyt.2020.546796moderateconsumed1 section
2020Use of UPLC-HRMS/MS for In Vitro and In Vivo Metabolite Identification of Three Methylphenidate-derived New Psychoactive SubstancesManier SK, Niedermeier S, Schäper J, Meyer MR · Journal of Analytical Toxicologydoi:10.1093/jat/bkz052moderateconsumed3 sections
2019Use of cognitive enhancers: methylphenidate and analogsCarlier J, Giorgetti R, Varì MR, Pirani F, Ricci G, Busardò FP · European Review for Medical and Pharmacological Sciencesdoi:10.26355/eurrev_201901_16741moderateconsumed1 section
2018Pharmacological profile of methylphenidate-based designer drugsLuethi D, Kaeser PJ, Brandt SD, Krähenbuhl S, Hoener MC, Liechti ME · Neuropharmacologydoi:10.1016/j.neuropharm.2017.08.020moderateconsumed2 sections
2018Tramadol: Understanding the Risk of Serotonin Syndrome and SeizuresHassamal S, Miotto K, Dale W, Danovitch I · The American Journal of Medicinedoi:10.1016/j.amjmed.2018.04.025moderateconsumed1 section
2017Analysis of six 'neuro-enhancing' phenidate analogsKlare H, Neudörfl JM, Brandt SD, Mischler E, Meier-Giebing S, Deluweit K, Westphal F, Laussmann T · Drug Testing and Analysisdoi:10.1002/dta.2161moderateconsumed1 section
2017Canada Gazette: Amendments to Controlled Drugs and Substances Act Schedule III (methylphenidate analogues)Health Canadaurl:e65534339fe76a9fweakconsumedcited only
2017UK control of methylphenidate-based NPS: Misuse of Drugs (Amendment) Regulations 2017UK Home Officeurl:249e0f66de3cb475weakconsumedcited only
2016Germany NpSG: New Psychoactive Substances Act (Neue-psychoaktive-Stoffe-Gesetz) November 2016German Federal Governmenturl:2c09a455e415ab0aweakconsumedcited only
2016Identification of in vitro metabolites of ethylphenidate by liquid chromatography coupled to quadrupole time-of-flight mass spectrometryNegreira N, Erratico C, van Nuijs AL, Covaci A · Journal of Pharmaceutical and Biomedical Analysisdoi:10.1016/j.jpba.2015.09.029moderateconsumed2 sections
2016Seven fatalities associated with ethylphenidate.Maskell PD, Smith PR, Cole R, Hikin L, Morley SR · Forensic Science Internationaldoi:10.1016/j.forsciint.2015.12.045weakconsumed2 sections
2015Novel psychoactive substances (designer drugs): overview and pharmacology of modulators of monoamine signalingLiechti ME · Swiss Medical Weeklydoi:10.4414/smw.2015.14043moderateconsumed3 sections
2015UK Temporary Class Drug Order: Methylphenidate-based NPS (ACMD Report, April 2015)Advisory Council on the Misuse of Drugs (ACMD)url:ec0798ba86d0bb86weakconsumedcited only
2015UNODC Early Warning Advisory: UK temporarily bans five methylphenidate-related NPS (April 2015)UNODCurl:cd066895e93f8534weakconsumedcited only
2014Ethylphenidate as a selective dopaminergic agonist and methylphenidate-ethanol transesterification biomarker.Patrick KS, Corbin TR, Murphy CE · Journal of Pharmaceutical Sciencesdoi:10.1002/jps.24202moderateconsumed1 section
2014Pharmacokinetic and pharmacodynamic effects of methylphenidate and MDMA administered alone or in combinationHysek CM, Simmler LD, Schillinger N, et al. · International Journal of Neuropsychopharmacologydoi:10.1017/s1461145713001132strongconsumedcited only
2013Differential influences of ethanol on early exposure to racemic methylphenidate compared with dexmethylphenidate in humansPatrick KS, Straughn AB, Reeves OT, Bernstein H, Bell GH, Anderson ER, Malcolm RJ · Drug Metabolism and Dispositiondoi:10.1124/dmd.112.048595moderateconsumed3 sections
2013Isopropylphenidate: an ester homolog of methylphenidate with sustained and selective dopaminergic activity and reduced drug interaction liabilityMarkowitz JS, Zhu HJ, Patrick KS · Journal of Child and Adolescent Psychopharmacologydoi:10.1089/cap.2013.0074moderateconsumed8 sections
2013Overdose of drugs for attention-deficit hyperactivity disorder: clinical presentation, mechanisms of toxicity, and management.Spiller HA, Hays HL, Aleguas A · CNS Drugsdoi:10.1007/s40263-013-0084-8moderateconsumed2 sections
2012US Patent US20120245201A1: Isopropylphenidate for Treatment of ADHD and Fatigue-Related DisordersMarkowitz JSurl:783650e749d86b22weakconsumedcited only
2009Tramadol: seizures, serotonin syndrome, and coadministered antidepressantsSansone RA, Sansone LA · Psychiatry (Edgmont)pmid:19724727moderateconsumed1 section
2007Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporterFroimowitz M, Gu Y, Dakin LA, et al. · Journal of Medicinal Chemistrypmid:17228864moderateconsumed1 section
1993A comparison of the motor-activating effects of acute and chronic exposure to amphetamine and methylphenidateMcNamara CG, Davidson ES, Schenk S · Pharmacology Biochemistry and Behaviorpmid:8332631moderateconsumed2 sections
—Searched ClinicalTrials.gov for "isopropylphenidate" — 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/isopropylphenidate/version/1
  2. 0022026-06-04proposal41 value proposals approved together

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

    41 items in this filing

    • contraindication · cardiovascular
    • contraindication · psychiatric
    • contraindication · psychiatric
    • contraindication · neurological
    • contraindication · metabolic
    • contraindication · other
    • contraindication · psychiatric
    • dose_tier · threshold
    • dose_tier · light
    • dose_tier · common
    • dose_tier · strong
    • dose_tier · heavy
    • toxicity
    • dependence · full
    • withdrawal
    • tolerance
    • dosage · oral
    • dosage · insufflated
    • duration · oral · onset
    • duration · oral · come_up
    • duration · oral · peak
    • duration · oral · offset
    • duration · oral · total
    • duration · oral · aftereffects
    • duration · insufflated · onset
    • duration · insufflated · come_up
    • duration · insufflated · peak
    • duration · insufflated · offset
    • duration · insufflated · total
    • duration · insufflated · aftereffects
    • timeline · oral · onset
    • timeline · oral · come_up
    • timeline · oral · peak
    • timeline · oral · resolution
    • timeline · oral · afterglow
    • timeline · insufflated · onset
    • timeline · insufflated · come_up
    • timeline · insufflated · peak
    • timeline · insufflated · resolution
    • timeline · insufflated · afterglow
    psx:substance/isopropylphenidate/proposal/contraindication/b165aa46-8301-4d0e-bb48-c0fe6beda9e2
  3. 0032026-06-04publicationPublication — backfill

5Issued documents

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

Issued documents
documentcontent hashissuedfrom versionsuperseded
info_cardab5c50b066ead54344c1b2cf…2026-10-19 20:32Revision 1current
emergency58d3299a8754d788e3d74c0e…2026-09-04 04:30Revision 1current
info_cardff3ab5c76728a750696a85e3…2026-09-04 04:30Revision 1superseded2026-10-19
noticedc91d6955c9b7fec24bc7863…2026-09-04 04:30Revision 1current