Drug intelligence / Profile preview

pyrazolam

Development stage
Discontinued
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Pyrazolam is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s. It was later "rediscovered" and sold as a designer drug since 2012. Pyrazolam is known for its anxiolytic and sedative properties and has structural similarities to alprazolam and bromazolam. Unlike many other benzodiazepines, pyrazolam does not appear to undergo metabolism; instead it is excreted unchanged in the urine. Its mechanism of action involves binding to GABA-A receptors in the brain—specifically with selectivity for α₂ and α₃ receptor subtypes—enhancing the inhibitory effects of gamma-aminobutyric acid (GABA), which results in calming effects on the central nervous system. Pyrazolam has been marketed for anxiety treatment but is not widely recognized or approved for clinical use; it remains controversial due to its recreational use and potential for abuse.[1][6][8]

Other names
pirazolam8-bromo-1-methyl-6-pyridin-2-yl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine[2][5]8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine[5]PYRAZOLAM (NFLIS-DRUG)[4]
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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