Pynazolam – Triazolobenzodiazepine Derivative (Research Use Only)
Overview
Pynazolam is a synthetic benzodiazepine derivative of the triazolo-benzodiazepine (TBZD) class. It was first described in the 1970s but was never developed for clinical use.
It has emerged in recent years as a “designer benzodiazepine” / novel psychoactive substance (NPS) and is of interest in forensic toxicology, GABA<sub>A</sub> receptor research, and structure-activity relationship (SAR) studies.
Chemical Identity & Structure
- IUPAC Name: 1-methyl-8-nitro-6-(pyridin-2-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
- Molecular Formula: C₁₆H₁₂N₆O₂
- CAS Number: 2034366-97-5
- Class: Triazolobenzodiazepine (TBZD)
- Appearance: Typically supplied as research grade powder or salt (analytical standard)
Mechanism of Action (Inference)
As a benzodiazepine analog, Pynazolam is presumed to act as a positive allosteric modulator of the GABA<sub>A</sub> receptor. By binding to the benzodiazepine site, it enhances GABA-mediated chloride flux, causing neuronal hyperpolarization and CNS depression.
Designer benzodiazepines of the TBZD class are known to exhibit strong sedative, anxiolytic, muscle-relaxant, hypnotic, and amnestic effects—though the precise pharmacology of Pynazolam remains largely uncharacterised.
Pharmacological & Toxicological Considerations
- There is limited published data on human pharmacokinetics or clinical use of Pynazolam. In silico and experimental modelling suggest high potency, and typical “designer benzodiazepine” risk profiles apply.
- Designer benzodiazepines have been implicated in hospitalisations, impaired driving, and fatalities—especially when used with opioids, alcohol or other depressants.
- Given the unknown therapeutic index and high potency, laboratory handling must assume narrow margin between effect and toxicity.
Analytical & Forensic Applications
Pynazolam can be used as a reference compound in:
- LC-MS/MS and GC-MS method validation for designer benzodiazepine detection
- Forensic toxicology screening of NPS-related intoxications
- SAR studies exploring how the 8-nitro and pyridinyl substitutions affect receptor binding and metabolism
Safety, Handling & Laboratory Precautions
- Use only in licensed, well-equipped laboratories
- Employ PPE: gloves, eye protection, respirator (if aerosol risk)
- Use analytical precision balances and avoid cross-contamination
- Dispose in compliance with institutional chemical hazard protocols
- Label clearly: For Analytical/Forensic Use Only – Not for Human Consumption
Legal & Regulatory Status
- Pynazolam is an unapproved psychoactive substance. Many jurisdictions regulate designer benzodiazepines under analogue laws or specific controls.
- Researchers must verify local controlled-substance classification and institutional compliance prior to acquisition or use.
Summary
Pynazolam is a potent triazolobenzodiazepine analogue with forensic and pharmacological significance. Its structural modifications (8-nitro group, pyridinyl substitution) make it relevant for GABA<sub>A</sub> receptor studies and designer benzodiazepine monitoring. Given its unknown human profile and high potency, it demands rigorous analytical handling and is strictly for research use.
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• white/yellowish powder
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