Chemistry

Pyrazolam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R1 and R4. Bromine is bound to this bicyclic structure at R7. Additionally, at R6 the bicylic core is substitued with a 2-pyridine ring. Pyrazolam also contains a 1-methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Pyrazolam belongs to a class of benzodiazepines containing this fused triazole ring, called triazolobenzodiazepines, distinguished by the suffix "-zolam".

Pharmacology

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors.[9] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of pyrazolam on the nervous system.

The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.[10]

Pyrazolam is most selective for the α2 and α3 receptor subtypes.[11] It is excreted by the body unchanged thus not interacting with liver enzymes like other benzodiazepines,[12] meaning that its use in people with reduced liver function may be safer.

Pyrazolam has structural similarities to alprazolam and bromazepam.[13] Unlike other benzodiazepines, pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine.[14] It is most selective for the α2 and α3 subtypes of the GABAA receptor.[15]

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