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psx:substance/pyrazolam/value/timeline/oral/onset@1

valuereferenced by edges — no row of its own

derived from · upstream

feeds · downstream

none recorded

Closure of psx:substance/pyrazolam/value/timeline/oral/onset@1: 1 upstream, 0 downstream.

psx:substance/pyrazolam/value/timeline/oral/onset@1
└─ derived_from  proposal/timeline/75b8f53b-568b-4f65-976a-20ba5bc388d2  timeline · oral · onset

indented by distance from this node, not by parentage

1Provenance card

the boundary, as counts

Sources

2624 with DOI

1 strong · 19 moderate · 6 weak

Compilations

12026-05-09T17:35:44.222Z

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

Decisions

31last ruled 2026-06-04

1 awaiting a ruling

Issued documents

42026-10-19T20:33:54.921Z

notice · info card · emergency

Searches

232 with no results

queries and counts on the build

Claims checked

7961 supported

61 supported · 18 not

Correspondence

0received

consent field ships in Phase 4

Edges

250

derivations recorded for this entity

Complete over 26 sources, 1 compilation, and 31 decisions.Not here: the private journal (never); 1 proposal awaiting a ruling (listed as pending only).Working material — drafts, discards, unsupported claims — is listed below and readable on the working page.Cite: psychedex.org/substances/pyrazolam/archive

2Build

one panel per compilation run

generation run 2026-05-09

86 min completedmodel pipeline-v5plan not recordedrun/e1b3873a…

Selection

results seen147
selected by the model46
consumed as sources26

Verification

claims checked79
supported57
partially supported4
not supported0
inconclusive18
  • record
  • seen / partial
  • working

The model's own caveats

  • structural_inference
  • sparse_evidence
  • safety_data_unverified

Reproduce

inputs
26 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
23 searches — query, source, results, what was kept and why
23 searches for this run
#sourcequeryseenkeptrationale
1OpenAlexpyrazolam benzodiazepine designer drug105Selected for citation ranking, historical context, and pharmacological scope
2PubMedpyrazolam pharmacology benzodiazepine1510Selected articles with direct pyrazolam data or closely relevant designer BZD data
3PubChempyrazolam11Used to verify chemical identity data from the brief
4ClinicalTrials.gov · absencepyrazolam00Confirms absence of formal clinical trial history
5PubMed · absencepyrazolam synthesis Fryer triazolo benzodiazepine 1980s00Will need to find via web search
6WebSearchpyrazolam GABA alpha subunit binding affinity Ki nM IC50 selectivity alpha2 alpha3 anxiolytic102GABA receptor pharmacology data
7WebSearchpyrazolam legal status scheduling United States UK EU DEA 2026103Legal status data not available in PubMed; web search necessary
8WebSearchpyrazolam Fryer synthesis 1970s 1980s American Cyanamid triazolo benzodiazepine original patent101Critical correction to assumed synthesis history
9WebSearchpyrazolam characterization serum urine Auwarter Moosmann 2013 research chemical101Primary characterization study with pharmacokinetic data
10PMC / Abouchedid 2018—13Specific pyrazolam pharmacokinetic and use-pattern data
11PubMedpyrazolam metabolism urine detection52Direct pyrazolam metabolism data
12Multiple sourcespyrazolam metabolism contradiction23Critical data contradiction requiring flagging
13WebSearchpyrazolam case report intoxication poisoning hospital clinical symptoms treatment101Only published pyrazolam-specific poisoning case report
14WebSearchpyrazolam Australia Canada legal status scheduled controlled102Legal status data
15PubChem CID 12562545CID 1256254511Chemical identity verification
16WebSearchpyrazolam CAS 39243-02-2 physical properties melting point101Physical properties not in academic literature
17PubMed8-Substituted triazolobenzodiazepines GABA pharmacology Cook Rowlett11Directly relevant structural analog pharmacology
18Multiplepyrazolam synthesis history original patent51Origin and synthesis history
19WebSearchpyrazolam CAS 39243-02-2 physical properties melting point density101Physical property data absent from academic literature
20WebSearchpyrazolam case report intoxication hospital clinical symptoms101Only pyrazolam-specific poisoning case report
21WebSearchpyrazolam alpha subunit GABA anxiolytic selectivity alpha2 alpha3 NOT euphoria most anxiolytic designer100Community/secondary evidence for subunit selectivity - no primary source found
22PubMedGABA alpha1 sedation alpha2 anxiolytic benzodiazepine subunit selective pharmacology52Mechanistic basis for pyrazolam alpha2/3 selectivity interpretation
23WebFetch—14UK use pattern and pharmacokinetic data
79 claims by section — every cited sentence, checked against its source
safety17 · 12 ok
  • The Magny 2026 poisoning involved co-ingestion with high-concentration ethanolsupported

    Vodka solution contained ethanol (330 g/L) and pyrazolam (450 mg/L). s11419-025-00750-3

  • Flumazenil was administered.supported

    Flumazenil administered. s11419-025-00750-3

  • Seven of 24 patients exposed only to NPS benzodiazepines required ICU admissionpartially supported

    Seven cases required ICU admission; responded to flumazenil. 15563650.2018.1510502

  • The single post-mortem case (Lehmann et al. 2019) involved pyrazolam (femoral blood 28 µg/L) in a polydrug death attributed to positional asphyxia, with co-detected diclazepam, 3-fluorophenmetrazine, amphetamine, and caffeinesupported

    Femoral blood pyrazolam 28 µg/L. Cause of death: positional asphyxia from poly-drug intoxication including designer benzodiazepines and synthetic stimulants. j.forsciint.2019.109959

  • Bäckberg et al. (2019) identified pyrazolam in clinical NPS benzodiazepine intoxication cases through the Swedish STRIDA projectsupported

    Bioanalytical and clinical data on NPS BZD intoxications from the Swedish STRIDA project. Pyrazolam detected in clinical intoxication cases. 15563650.2018.1506130

  • Høiseth et al. (2016) detected pyrazolam in blood from drugged drivers and criminal offenders in Norway, correlating blood levels with clinical impairment.supported

    Blood concentrations of new designer benzodiazepines in drugged drivers and criminal offenders; relates concentrations to clinical impairment. j.forsciint.2016.09.006

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • All characterizations derive from benzodiazepine class pharmacology.supported

    Review of NPS benzodiazepines; covers PK parameters, metabolic pathways, analytical methods; notes pyrazolam among first commercial NPS BZDs. dta.2211

  • Claim in safety — inconclusiveinconclusiveworking →

  • Claim in safety — inconclusiveinconclusiveworking →

  • A published case report of designer benzodiazepine (bromazolam) detoxification via diazepam substitution and gradual taper provides a template approachsupported

    23-year-old woman admitted for detoxification from designer BZD bromazolam. Daily use 6 mg bromazolam converted to 20 mg diazepam. Fixed-dose and symptom-triggered regimen. Tapered without complications. 10550887.2024.2365006

  • The benzodiazepine class is characterized as having high potential for both physical and psychological dependence.supported

    Neurobiological and pharmacologic properties result in high potential for misuse and physical dependence. j.mcna.2021.08.012

  • Claim in safety — inconclusiveinconclusiveworking →

  • The Lehmann 2019 fatality involved pyrazolam combined with diclazepam and stimulants.supported

    Cause of death: positional asphyxia from poly-drug intoxication including designer benzodiazepines and synthetic stimulants. j.forsciint.2019.109959

  • However, the Moosmann data suggesting minimal metabolism imply this interaction pathway may be of limited significance for pyrazolam specifically.supported

    No detectable metabolites in serum/urine. Excreted largely unchanged. s11419-013-0187-4

  • Stimulant combinations: Abouchedid et al. (2018) found that 16.1% of pyrazolam-related forum discussions concerned use as a stimulant comedown aidpartially supported

    Primary motivations: anxiolysis 53%, sedation/sleep 11%, stimulant withdrawal 10.1%, euphoria 6.1%, functional capacity 8.5%. s13181-018-0659-3

pharmacology14 · 13 ok
  • It binds at the classical benzodiazepine site located at the α+/γ2− subunit interface, enhancing the inhibitory effect of endogenous GABA by increasing the frequency of chloride ion channel opening without directly gating the channel.supported

    In vitro γ-aminobutyric acid A (GABAA) receptor activity and binding interactions at the α+/γ2– interface of 53 prescription and designer benzodiazepines s42004-026-02001-x

  • This subtype selectivity profile has functional consequences: α1-mediated effects include sedation, amnesia, and ataxia, while α2 and α3 subunits mediate anxiolysis and, to a lesser extent, muscle relaxationsupported

    α1 mediates sedation; α2/α3 mediate anxiolysis; α5 associated with cognitive effects. α2/α3-selective PAMs developed as non-sedating anxiolytics. acs.jmedchem.9b01312

  • Claim in pharmacology — inconclusiveinconclusiveworking →

  • The α2/α3 selectivity claim rests on three converging lines of evidence: (1) the 2026 in vitro GABA-A receptor study characterizing 53 benzodiazepines at α1β2γ2 assemblies, which found pyrazolam to be equally potent as bromazolam but significantly less efficacious — consistent with partial or subtype-selective engagement at α1; (2) structure-activity data from Golani et al., who demonstrated that the closely related compound SH-TRI-108 (differing from pyrazolam only at the 8-position: 8-ethynyl vs. 8-bromo) exhibited a 25-fold functional potency difference between α1β3γ2 and α2β3γ2 subtypes; and (3) the subjective effects profile reported by users, which consistently identifies pronounced anxiolysis with limited sedation, a pattern mechanistically consistent with α2/α3-preferring compounds.supported

    Pyrazolam (compound 38) was equally as potent as bromazolam but significantly less efficacious. Positive allosteric modulators show wide variation in potency and efficacy. s42004-026-02001-x

  • The α2/α3 selectivity claim rests on three converging lines of evidence: (1) the 2026 in vitro GABA-A receptor study characterizing 53 benzodiazepines at α1β2γ2 assemblies, which found pyrazolam to be equally potent as bromazolam but significantly less efficacious — consistent with partial or subtype-selective engagement at α1; (2) structure-activity data from Golani et al., who demonstrated that the closely related compound SH-TRI-108 (differing from pyrazolam only at the 8-position: 8-ethynyl vs. 8-bromo) exhibited a 25-fold functional potency difference between α1β3γ2 and α2β3γ2 subtypes; and (3) the subjective effects profile reported by users, which consistently identifies pronounced anxiolysis with limited sedation, a pattern mechanistically consistent with α2/α3-preferring compounds.supported

    SH-TRI-108 (8-ethynyl-1-methyl-6-(pyridin-2-yl) analog of pyrazolam) showed 25-fold functional potency difference between α1 and α2 subtypes. fphar.2021.625233

  • The sole published human pharmacokinetic data for pyrazolam derive from a self-administration study by Moosmann et al. (2013), in which one of the authors ingested 1 mg orally (two 0.5 mg tablets).supported

    Self-administration study (1 mg oral): elimination half-life ~17 hours (vendor claimed 6h). s11419-013-0187-4

  • The elimination half-life was approximately 17 hourssupported

    elimination half-life ~17 hours (vendor claimed 6h) s11419-013-0187-4

  • The elimination half-life was approximately 17 hourssupported

    Half-life ~17h (3x longer than vendor-advertised). s13181-018-0659-3

  • This value is substantially longer than the 6-hour half-life advertised by vendors at the time of the study — a discrepancy noted explicitly by Abouchedid et al.supported

    Half-life ~17h (3x longer than vendor-advertised). s13181-018-0659-3

  • Pyrazolam remained detectable in serum for more than 50 hours and in urine for up to 6 days following a single 1 mg dose.supported

    Detectable in serum >50h, urine up to 6 days. s11419-013-0187-4

  • Moosmann et al. (2013) detected no metabolites in serum or urine after their 1 mg self-administration, concluding that pyrazolam is excreted largely unchangedsupported

    No detectable metabolites in serum/urine. Excreted largely unchanged. s11419-013-0187-4

  • Pettersson Bergstrand et al. (2018), analyzing urine from real-world intoxication cases, identified a parent glucuronide as the most abundant urinary metabolite, alongside mono-hydroxy metabolites and their glucuronide conjugatessupported

    Main urinary metabolites of pyrazolam: parent glucuronide, mono-hydroxy metabolites, mono-hydroxy glucuronides. Parent glucuronide is the most common metabolite without enzymatic hydrolysis. dta.2243

  • A subsequent in vitro study by the same group (2019), using pooled human liver microsomes, failed to detect UGT1A4- or other UGT-mediated glucuronidation of pyrazolamsupported

    Pyrazolam glucuronides were not detected in incubations with individual UGTs or pooled human liver microsomes, suggesting no significant direct glucuronidation. dta.2463

  • The blood-to-plasma ratio was addressed by Manchester et al. (2022) in a QSAR study of designer benzodiazepines, though the specific numerical value for pyrazolam was not extracted from the available abstract.supported

    Blood-to-plasma ratio and QSAR-predicted GABA-A receptor binding affinity for multiple designer BZDs. s11419-022-00616-y

summary11 · 8 ok
  • Pyrazolam (8-bromo-1-methyl-6-pyridin-2-yl-4H-triazolo-benzodiazepine) is a triazolobenzodiazepine derivative and positive allosteric modulator of the GABA-A receptor, active at oral doses of 0.5–3 mg with a subjective effects duration of 5–8 hourspartially supported

    Recreational doses 0.5-4mg. Half-life ~17h (3x longer than vendor-advertised). s13181-018-0659-3

  • Claim in summary — inconclusiveinconclusiveworking →

  • It resurfaced in 2012 as one of the earliest designer benzodiazepines sold through online research chemical vendors, an event that Moosmann et al. described as marking "the beginning of designer benzodiazepines being sold as recreational drugs or self-medication"supported

    Documents that pyrazolam appeared on internet shops selling research chemicals in 2012, marking the beginning of designer BZDs sold as recreational drugs. jms.3279

  • Claim in summary — inconclusiveinconclusiveworking →

  • Pyrazolam acts at the classical benzodiazepine binding site at the α+/γ2− interface of GABA-A receptorssupported

    In vitro γ-aminobutyric acid A (GABAA) receptor activity and binding interactions at the α+/γ2– interface of 53 prescription and designer benzodiazepines s42004-026-02001-x

  • Structure-activity studies of closely related 8-substituted triazolobenzodiazepines demonstrate that modifications at the 8-position modulate α1 subunit engagement, providing a mechanistic basis for pyrazolam's anxiolytic-selective profilesupported

    SH-TRI-108 showed 25-fold functional potency difference between α1 and α2 subtypes. 8-position substitution affects α1 C-loop binding. fphar.2021.625233

  • As a GABA-A positive allosteric modulator, the compound carries the class-wide risk profile of respiratory depression when combined with other CNS depressants — the single published fatality involving pyrazolam was a polydrug death attributed to positional asphyxiasupported

    Cause of death: positional asphyxia from poly-drug intoxication including designer benzodiazepines and synthetic stimulants. j.forsciint.2019.109959

  • Claim in summary — inconclusiveinconclusiveworking →

  • The pharmacokinetic profile remains incompletely characterized: a single self-administration study established an elimination half-life of approximately 17 hours, but the metabolic fate of pyrazolam is the subject of an unresolved three-way contradiction in the published literature.supported

    Self-administration study (1 mg oral): elimination half-life ~17 hours (vendor claimed 6h). No detectable metabolites in serum/urine. Excreted largely unchanged. s11419-013-0187-4

  • The pharmacokinetic profile remains incompletely characterized: a single self-administration study established an elimination half-life of approximately 17 hours, but the metabolic fate of pyrazolam is the subject of an unresolved three-way contradiction in the published literature.supported

    Main urinary metabolites of pyrazolam: parent glucuronide, mono-hydroxy metabolites, mono-hydroxy glucuronides. Parent glucuronide is the most common metabolite without enzymatic hydrolysis. dta.2243

  • The pharmacokinetic profile remains incompletely characterized: a single self-administration study established an elimination half-life of approximately 17 hours, but the metabolic fate of pyrazolam is the subject of an unresolved three-way contradiction in the published literature.supported

    Pyrazolam glucuronides were not detected in incubations with individual UGTs or pooled human liver microsomes, suggesting no significant direct glucuronidation. dta.2463

pharmacokinetic-detail9 · 7 ok
  • These values derive from a single self-administration study (n = 1, dose = 1 mg oral)supported

    Self-administration study (1 mg oral): elimination half-life ~17 hours (vendor claimed 6h). s11419-013-0187-4

  • Femoral blood concentration was 28 µg/L (28 ng/mL) in a polydrug death involving pyrazolam, diclazepam, 3-fluorophenmetrazine, amphetamine, and caffeinesupported

    Femoral blood pyrazolam 28 µg/L. Higher concentrations in tissues than blood. Cause of death: positional asphyxia from poly-drug intoxication including designer benzodiazepines and synthetic stimulants. j.forsciint.2019.109959

  • Claim in pharmacokinetic-detail — inconclusiveinconclusiveworking →

  • Claim in pharmacokinetic-detail — inconclusiveinconclusiveworking →

  • Vendors advertised a half-life of approximately 6 hours at the time pyrazolam entered the market — roughly three times shorter than the measured valuesupported

    Half-life ~17h (3x longer than vendor-advertised). s13181-018-0659-3

  • The authors concluded that pyrazolam is excreted largely in unchanged form.supported

    Excreted largely unchanged. s11419-013-0187-4

  • In vitro incubation of pyrazolam with pooled human liver microsomes expressing UDP-glucuronosyltransferases (UGTs) failed to produce detectable glucuronide conjugates, including via UGT1A4 — the enzyme most commonly responsible for N-glucuronidation of benzodiazepinessupported

    Pyrazolam glucuronides were not detected in incubations with individual UGTs or pooled human liver microsomes, suggesting no significant direct glucuronidation. Metabolism of related DBZDs primarily via UGT1A4. dta.2463

  • In the 2026 acute poisoning case reported by Magny et al., plasma pyrazolam concentration was 500 ng/mL at 5 hours post-ingestion, declining to 270 ng/mL at 72 hourssupported

    Plasma pyrazolam 500 ng/mL at 5h post-ingestion, decreasing to 270 ng/mL at 72h. s11419-025-00750-3

  • Confirmatory identification requires LC-MS/MS or LC-HRMSsupported

    LC-HRMS method for 28 NPS BZDs in urine. Pyrazolam detected in patient urine samples. j.clinms.2018.08.004

clinical-evidence6 · 6 ok
  • The sole controlled human exposure data derive from the Moosmann et al. (2013) self-administration study, in which a single investigator ingested 1 mg orally and provided serial blood and urine samples for pharmacokinetic analysissupported

    Self-administration study (1 mg oral): elimination half-life ~17 hours (vendor claimed 6h). No detectable metabolites in serum/urine. s11419-013-0187-4

  • Abouchedid et al. (2018) analyzed online forum posts to characterize availability, cost, and user motivations for pyrazolam use in the UK, identifying anxiolysis as the primary self-reported motivation (53% of coded posts) and documenting recreational dose ranges of 0.5–4 mg.supported

    Recreational doses 0.5-4mg. Primary motivations: anxiolysis 53%, sedation/sleep 11%, stimulant withdrawal 10.1%, euphoria 6.1%, functional capacity 8.5%. s13181-018-0659-3

  • Høiseth et al. (2016) detected pyrazolam in blood samples from drugged drivers and criminal offenders in Norway, correlating blood concentrations with clinical impairment.supported

    Blood concentrations of new designer benzodiazepines in drugged drivers and criminal offenders; relates concentrations to clinical impairment. j.forsciint.2016.09.006

  • The compound has never been approved as a pharmaceutical product in any jurisdiction and has never entered formal clinical development.supported

    Review of NPS benzodiazepines; notes pyrazolam among first commercial NPS BZDs. dta.2211

  • The compound has never been approved as a pharmaceutical product in any jurisdiction and has never entered formal clinical development.supported

    Pyrazolam among first designer BZDs online alongside diclazepam and flubromazepam. wps.20236

  • Bäckberg et al. (2019) identified pyrazolam in clinical intoxication cases through the Swedish STRIDA project, providing emergency department presentation data.supported

    Bioanalytical and clinical data on NPS BZD intoxications from the Swedish STRIDA project. Pyrazolam detected in clinical intoxication cases. 15563650.2018.1506130

comparative-pharmacology5 · 3 ok
  • Pyrazolam requires doses in the 0.75–3 mg range for comparable subjective intensity, and the qualitative character differs — users consistently describe pyrazolam's effects as more "functional" and less cognitively impairing at anxiolytic-equivalent doses.partially supported

    Recreational doses 0.5-4mg. Primary motivations: anxiolysis 53%, sedation/sleep 11%, stimulant withdrawal 10.1%, euphoria 6.1%, functional capacity 8.5%. s13181-018-0659-3

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • In the 2026 α1β2γ2 GABA-A receptor assay, pyrazolam demonstrated potency equivalent to bromazolam but significantly lower efficacysupported

    Pyrazolam (compound 38) was equally as potent as bromazolam but significantly less efficacious. s42004-026-02001-x

  • Claim in comparative-pharmacology — inconclusiveinconclusiveworking →

  • Pyrazolam's metabolic fate remains unresolved, but the Moosmann data suggesting minimal hepatic metabolism would, if confirmed, represent a clinically meaningful departure from the metabolic profile of its closest structural relativesupported

    No detectable metabolites in serum/urine. Excreted largely unchanged. s11419-013-0187-4

history5 · 3 ok
  • Pyrazolam resurfaced in approximately 2012 when it appeared for sale through online vendors marketing "research chemicals." Moosmann et al. documented this emergence in a 2013 publication on flubromazepam, explicitly noting: "The appearance of pyrazolam in Internet shops selling 'research chemicals' in 2012 marked the beginning of designer benzodiazepines being sold as recreational drugs or 'self medication'"supported

    Documents that pyrazolam appeared on internet shops selling research chemicals in 2012, marking the beginning of designer BZDs sold as recreational drugs. jms.3279

  • Pyrazolam, diclazepam, and flubromazepam constituted the first wave of designer benzodiazepines available onlinesupported

    Pyrazolam among first designer BZDs online alongside diclazepam and flubromazepam. wps.20236

  • Claim in history — inconclusiveinconclusiveworking →

  • Claim in history — inconclusiveinconclusiveworking →

  • The United Kingdom classified pyrazolam as a Class C, Schedule 2 substance under the Misuse of Drugs Act 1971 in June 2017, alongside diclazepam, flubromazepam, and etizolamsupported

    Classified Class C, Schedule 2 since June 2017 in UK. s13181-018-0659-3

neuroscience5 · 4 ok
  • Claim in neuroscience — inconclusiveinconclusiveworking →

  • Pyrazolam represents a de facto probe of the anxioselective hypothesis — the proposition that anxiolysis can be pharmacologically separated from sedation, amnesia, and abuse liability through subtype-selective GABA-A modulationsupported

    α2/α3-selective PAMs developed as non-sedating anxiolytics. acs.jmedchem.9b01312

  • Pyrazolam, as an unintentionally subtype-preferring compound used extensively in non-clinical settings, provides indirect human evidence for the validity of the concept — users consistently report the predicted dissociation of anxiolysis from sedation and euphoria.supported

    Primary motivations: anxiolysis 53%, sedation/sleep 11%, euphoria 6.1%. s13181-018-0659-3

  • Metabolic pathway resolution: Does pyrazolam undergo glucuronidation in vivo, and if so, by which UGT isoform? The three-way contradiction in the published literature requires resolution — ideally through a controlled human pharmacokinetic study with modern analytical sensitivity.supported

    No detectable metabolites in serum/urine. Excreted largely unchanged. s11419-013-0187-4

  • Metabolic pathway resolution: Does pyrazolam undergo glucuronidation in vivo, and if so, by which UGT isoform? The three-way contradiction in the published literature requires resolution — ideally through a controlled human pharmacokinetic study with modern analytical sensitivity.supported

    Main urinary metabolites of pyrazolam: parent glucuronide, mono-hydroxy metabolites, mono-hydroxy glucuronides. dta.2243

receptor-pharmacology5 · 4 ok
  • The binding site is located at the interface between the α and γ2 subunits (α+/γ2− interface).supported

    In vitro γ-aminobutyric acid A (GABAA) receptor activity and binding interactions at the α+/γ2– interface of 53 prescription and designer benzodiazepines s42004-026-02001-x

  • The most informative in vitro data come from a 2026 study that characterized 53 prescription and designer benzodiazepines in a standardized α1β2γ2 GABA-A receptor assaysupported

    In vitro GABA-A receptor activity assay of 53 benzodiazepines. s42004-026-02001-x

  • Golani et al. (2021) systematically studied 8-substituted triazolobenzodiazepine analogs sharing pyrazolam's core scaffoldsupported

    8-substituted analogs of triazolam (same scaffold as pyrazolam) evaluated for GABA-A subtype selectivity. fphar.2021.625233

  • A compound with low α1 efficacy and preserved α2/α3 activity would be predicted to produce anxiolysis with attenuated sedation, amnesia, and euphoria — precisely the profile that users and analysts consistently attribute to pyrazolam.supported

    Primary motivations: anxiolysis 53%, sedation/sleep 11%, stimulant withdrawal 10.1%, euphoria 6.1%, functional capacity 8.5%. s13181-018-0659-3

  • Claim in receptor-pharmacology — inconclusiveinconclusiveworking →

chemistry1 · 0 ok
  • Claim in chemistry — inconclusiveinconclusiveworking →

effects-overview1 · 1 ok
  • The anxiolytic effect is described as "clean" or "pure" — a reduction of baseline anxiety without the accompanying euphoria, heavy sedation, or cognitive fog associated with non-selective benzodiazepines such as alprazolam or clonazolamsupported

    Primary motivations: anxiolysis 53%, sedation/sleep 11%, stimulant withdrawal 10.1%, euphoria 6.1%, functional capacity 8.5%. s13181-018-0659-3

3Sources

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

Sources
yearsourcetierstatusfeeds
2026An unusual way of acute Pyrazolam poisoning in consumer of commercially approved benzodiazepinesMagny R, Boukerma AK, Mihoubi A, Labat L, Houzé P · Forensic Toxicologydoi:10.1007/s11419-025-00750-3weakconsumed2 sections
2026In vitro γ-aminobutyric acid A (GABAA) receptor activity and binding interactions at the α+/γ2– interface of 53 prescription and designer benzodiazepinesNot specified in web search results · Communications Chemistry (Nature)doi:10.1038/s42004-026-02001-xweakconsumed4 sections
2025Clinical detoxification of bromazolam using diazepam: a case reportBuitenhuis D, Herdes DP, Verboeket SO · Journal of Addictive Diseasesdoi:10.1080/10550887.2024.2365006weakconsumed1 section
2024Benzodiazepine Boom: Tracking Etizolam, Pyrazolam, and Flubromazepam from Pre-UK Psychoactive Act 2016 to Present Using Analytical and Social Listening TechniquesMullin A, Scott M, Vaccaro G, Floresta G, Arillotta D, Catalani V, Corkery JM, Stair JL, Schifano F, Guirguis A · Pharmacy (Basel)doi:10.3390/pharmacy12010013moderateconsumedcited only
2024Physical properties of pyrazolam (CAS 39243-02-2)ChemicalBookurl:bf4c516406801f0fweakconsumedcited only
2023The Evolution Toward Designer Benzodiazepines in Drug-Facilitated Sexual Assault CasesPérez Orts M, van Asten A, Köhler I · Journal of Analytical Toxicologydoi:10.1093/jat/bkac017moderateconsumed1 section
2022Benzodiazepines and Related Sedatives.Peng L, Morford KL, Levander XA · Medical Clinics of North Americadoi:10.1016/j.mcna.2021.08.012moderateconsumed1 section
2022Fast and Sensitive Method for the Determination of 17 Designer Benzodiazepines in Hair by Liquid Chromatography-Tandem Mass SpectrometryDeFreitas L, Fonseca Pego AM, Kronstrand R, Lendoiro E, de Castro-Rios A, Concheiro M · Journal of Analytical Toxicologydoi:10.1093/jat/bkac044moderateconsumedcited only
2022The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepinesManchester KR, Waters L, Haider S, Maskell PD · Forensic Toxicologydoi:10.1007/s11419-022-00616-ymoderateconsumed1 section
20218-Substituted Triazolobenzodiazepines: In Vitro and In Vivo Pharmacology in Relation to Structural Docking at the α1 Subunit-Containing GABAA ReceptorGolani LK, Platt DM, Rüedi-Bettschen D, Edwanker C, Huang S, Poe MM, Furtmüller R, Sieghart W, Cook JM, Rowlett JK · Frontiers in Pharmacologydoi:10.3389/fphar.2021.625233moderateconsumed3 sections
2020'New/Designer Benzodiazepines': An Analysis of the Literature and Psychonauts' Trip ReportsOrsolini L, Corkery JM, Chiappini S, Guirguis A, Vento A, et al. · Current Neuropharmacologydoi:10.2174/1570159x18666200110121333moderateconsumedcited only
2020Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABAAR) Modulators Acting at the Benzodiazepine Binding Site: An UpdateMaramai S, Benchekroun M, Ward SE, Atack JR · Journal of Medicinal Chemistrydoi:10.1021/acs.jmedchem.9b01312strongconsumed2 sections
2019Designer benzodiazepines: a report of exposures recorded in the National Poison Data System, 2014-2017.Carpenter JE, Murray BP, Dunkley C, Kazzi ZN, Gittinger MH · Clinical Toxicologydoi:10.1080/15563650.2018.1510502moderateconsumed1 section
2019In vitro glucuronidation of designer benzodiazepines by human UDP-glucuronyltransferasesPettersson Bergstrand M, Richter LHJ, Maurer HH, Wagmann L, Meyer MR · Drug Testing and Analysisdoi:10.1002/dta.2463moderateconsumed3 sections
2019Occurrence and time course of NPS benzodiazepines in Sweden - results from intoxication cases in the STRIDA project.Bäckberg M, Pettersson Bergstrand M, Beck O, Helander A · Clinical Toxicologydoi:10.1080/15563650.2018.1506130moderateconsumed2 sections
2019Organ distribution of diclazepam, pyrazolam and 3-fluorophenmetrazineLehmann S, Sczyslo A, Froch-Cortis J, Rothschild MA, Thevis M, Andresen-Streichert H, Mercer-Chalmers-Bender K · Forensic Science Internationaldoi:10.1016/j.forsciint.2019.109959weakconsumed3 sections
2018Assessment of the Availability, Cost, and Motivations for Use over Time of the New Psychoactive Substances-Benzodiazepines Diclazepam, Flubromazepam, and Pyrazolam-in the UKAbouchedid R, Gilks T, Dargan PI, Archer JRH, Wood DM · Journal of Medical Toxicologydoi:10.1007/s13181-018-0659-3moderateconsumed10 sections
2018Human urinary metabolic patterns of the designer benzodiazepines flubromazolam and pyrazolam studied by liquid chromatography-high resolution mass spectrometryPettersson Bergstrand M, Meyer MR, Beck O, Helander A · Drug Testing and Analysisdoi:10.1002/dta.2243moderateconsumed3 sections
2018The emergence of new psychoactive substance (NPS) benzodiazepines: A review.Manchester KR, Lomas EC, Waters L, Dempsey FC, Maskell PD · Drug testing and analysisdoi:10.1002/dta.2211moderateconsumed4 sections
2018Urine analysis of 28 designer benzodiazepines by liquid chromatography-high-resolution mass spectrometryPettersson Bergstrand M, Beck O, Helander A · Clinical Mass Spectrometrydoi:10.1016/j.clinms.2018.08.004moderateconsumed1 section
2017Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assaysPettersson Bergstrand M, Helander A, Hansson T, Beck O · Drug Testing and Analysisdoi:10.1002/dta.2003moderateconsumedcited only
2016Blood concentrations of new designer benzodiazepines in forensic cases.Høiseth G, Skogstad Tuv S, Karinen R · Forensic Science Internationaldoi:10.1016/j.forsciint.2016.09.006moderateconsumed2 sections
2015Designer benzodiazepines: A new challengeMoosmann B, King LA, Auwärter V · World Psychiatrydoi:10.1002/wps.20236moderateconsumed6 sections
2013Characterization of the designer benzodiazepine pyrazolam and its detectability in human serum and urineMoosmann B, Hutter M, Huppertz L, Ferlaino S, Redlingshöfer L, Auwärter V · Forensic Toxicologydoi:10.1007/s11419-013-0187-4moderateconsumed7 sections
2013Detection and identification of the designer benzodiazepine flubromazepam and preliminary data on its metabolism and pharmacokineticsMoosmann B, Huppertz LM, Hutter M, Buchwald A, Ferlaino S, Auwärter V · Journal of Mass Spectrometrydoi:10.1002/jms.3279moderateconsumed2 sections
1976US Patent 3,954,728: Preparation of 6-pyridyl-4H-triazolo[4,3-a][1,4]benzodiazepinesSternbach LH, Walser Aurl:9ab41e7091782867weakconsumedcited only
—Searched ClinicalTrials.gov for "pyrazolam" — no resultsabsenceno results—
—Searched PubMed for "pyrazolam synthesis Fryer triazolo benzodiazepine 1980s" — no resultsabsenceno results—

4Docket

one filing per activity — decisions, correspondence, reports

awaiting ruling — 1

  • dependence · taper2026-07-03
  1. 0012026-05-09revisionRevision 1

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

    psx:substance/pyrazolam/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 · other
    • contraindication · psychiatric
    • contraindication · hepatic
    • contraindication · pregnancy_breastfeeding
    • contraindication · neurological
    • contraindication · other
    • 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
    • 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
    psx:substance/pyrazolam/proposal/contraindication/b692a232-f691-4128-82a1-1f2d198741d9
  3. 0032026-06-04publicationPublication — backfill

5Issued documents

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

Issued documents
documentcontent hashissuedfrom versionsuperseded
info_card098392316a3d2e5bbbb25ea5…2026-10-19 20:33Revision 1current
emergencydcd2ca271fbe095dc7fb6211…2026-09-04 04:32Revision 1current
info_cardefade1856aafdedd85fa2c00…2026-09-04 04:32Revision 1superseded2026-10-19
notice7b3f31d0cd56d844640b8e27…2026-09-04 04:32Revision 1current