Pyrazolam

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A benzodiazepine derivative


Pyrazolam
File:Pyrazolam structure.png
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
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Legal status
CAS Number 39241-27-5
PubChem 9827100
DrugBank
ChemSpider 8003030
KEGG


Pyrazolam is a benzodiazepine derivative that was first synthesized in the 1970s. It is known for its anxiolytic properties and is used primarily in research settings. Unlike many other benzodiazepines, pyrazolam is not commonly prescribed for therapeutic use.

Chemical Structure and Properties[edit | edit source]

Pyrazolam belongs to the triazolobenzodiazepine class, which is characterized by the fusion of a triazole ring to the benzodiazepine structure. The chemical formula for pyrazolam is C16H12BrN5. It is structurally related to other benzodiazepines such as alprazolam and bromazepam.

Pharmacology[edit | edit source]

Pyrazolam acts as a positive allosteric modulator of the [[GABAA receptor]], which enhances the effect of the neurotransmitter gamma-aminobutyric acid (GABA). This action results in increased inhibitory neurotransmission in the brain, leading to its anxiolytic effects. Pyrazolam has a high affinity for the benzodiazepine site on the GABAA receptor, which contributes to its potency.

Effects[edit | edit source]

The primary effects of pyrazolam include:

  • Anxiolytic: Reduction of anxiety and stress.
  • Sedative: Induction of calmness and relaxation.
  • Muscle relaxant: Reduction of muscle tension.

Unlike some other benzodiazepines, pyrazolam is reported to have minimal hypnotic effects, making it less likely to induce sleep.

Usage[edit | edit source]

Pyrazolam is not approved for medical use in most countries and is primarily used in research settings to study the effects of benzodiazepines on the central nervous system. It is sometimes encountered in the designer drug market, where it is sold as a research chemical.

Legal Status[edit | edit source]

The legal status of pyrazolam varies by country. In some jurisdictions, it is classified as a controlled substance, while in others, it remains unscheduled. Researchers and users should be aware of the legal implications of possessing or using pyrazolam in their respective regions.

Safety and Toxicity[edit | edit source]

As with other benzodiazepines, the use of pyrazolam carries the risk of dependence and withdrawal symptoms. Overdose can lead to severe central nervous system depression, respiratory depression, and potentially fatal outcomes. Caution is advised when using pyrazolam, especially in combination with other central nervous system depressants such as alcohol or opioids.

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Contributors: Prab R. Tumpati, MD