Pyrazolam 2.5 MG Pellets

PRODUCT DESCRIPTION

Introduction

Pyrazolam is a benzodiazepine derivative, structurally classified as a triazolobenzodiazepine. It is known for its potent anxiolytic and sedative properties and is chemically related to alprazolam and bromazepam. Pyrazolam is distinctive among benzodiazepines because it is excreted largely unchanged and does not undergo extensive metabolism. Pyrazolam 2.5 mg pellets provide a precise, research-grade solid dosage form for studying its pharmacology, pharmacokinetics, and receptor interactions in controlled laboratory environments.

Chemical Properties and Specifications

Structural and Molecular Characteristics

• Chemical Formula: C16H12BrN5C16H12BrN5

• Molecular Weight: 354.20 g/mol

• CAS Number: 39243-02-2

• IUPAC Name: 8-bromo-1-methyl-6-(pyridin-2-yl)-4H-triazolo[4,3-a]benzodiazepine

• Synonyms: Pyrazolam, SH-I-04, Pirazolam

Physical Properties and Purity Standards

• Appearance: White crystalline solid or pellet form (2.5 mg per pellet)

• Purity: Typically ≥98% pure for research grade

• Melting Point: 253-255 °C

• Solubility:

  • DMF: 30 mg/mL

  • DMF:PBS (pH 7.2) 1:1: 0.5 mg/mL

  • DMSO: 20 mg/mL

  • Ethanol: 10 mg/mL

• Storage Recommendations: Store sealed at -20°C under inert atmosphere to preserve stability

Pharmacological Profile and Mechanism of Action

Proposed Mechanism of Action

Pyrazolam acts as a positive allosteric modulator of the GABAAA receptor, particularly selective for the α2 and α3 receptor subtypes. By potentiating GABAergic inhibition in the CNS, it produces sedative, anxiolytic, and muscle-relaxant effects. Pyrazolam’s pharmacokinetics are unique in that it resists metabolism and is excreted unchanged in urine, which could minimize liver burden and drug interactions.

Research Applications

Pyrazolam is widely used in research to investigate selective GABA receptor modulation, benzodiazepine pharmacology, and potential therapeutic applications in anxiety and sleep disorders. Its long half-life and metabolic profile also make it useful for forensic and toxicological studies.

Comparative Analysis with Related Compounds

Compare to Related Compounds

Compared to alprazolam and bromazepam, Pyrazolam displays similar anxiolytic potency but distinct pharmacokinetics. Unlike many benzodiazepines, Pyrazolam’s lack of active metabolites is its pharmacological hallmark, reducing cumulative drug effects.

Advantages for Research

Its unique metabolism and receptor selectivity provide a valuable experimental model for studying α2/α3-selective benzodiazepine effects and non-hepatic clearance mechanisms.

Safety and Handling Guidelines

Laboratory Safety

Use gloves, eye protection, and lab coats while handling Pyrazolam. Avoid inhalation and ingestion. Store securely to prevent unauthorized access.

Disposal and Environmental Considerations

Dispose of per hazardous chemical and pharmaceutical waste protocols to avoid environmental contamination.

Regulatory Status

Pyrazolam is classified as a research chemical and is controlled in many regions. It is not approved for clinical use in most countries and is strictly for laboratory research.

Frequently Asked Questions (FAQs)

1. What is the typical dose for research purposes?
   Common investigative doses range around 2.5 mg pellets for controlled study.

2. How soluble is Pyrazolam?
   Soluble in DMF, DMSO, and ethanol as specified above.

3. What are the storage requirements?
   Store sealed at -20°C, in an inert atmosphere, dry and protected from light.

4. How does Pyrazolam differ metabolically?
   It is excreted unchanged, lacking active metabolites common in benzodiazepines.

5. Is Pyrazolam safe to handle?
   Standard lab safety precautions apply.

Conclusion

Pyrazolam 2.5 mg pellets provide a high-purity, precise dosage form benzodiazepine for focused research into selective GABA receptor modulation, pharmacokinetics, and potential therapeutic profiles.