Bromazolam 4mg Pellets

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Bromazolam is a benzodiazepine derivative that was first synthesized in 1976 but has never been marketed for medical use. As a result, it is not available as a prescription medication and remains classified as a research chemical. Despite its lack of approval for medical applications, bromazolam has garnered interest within the research community due to its potential psychoactive effects.

Specifications and Chemical Information

The IUPAC name for bromazolam is 8-bromo-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine. It is identified by the CAS number 71368-80-4 and has a PubChem ID of 12562546. Commonly referenced names for bromazolam include Bromazola, bromazolon, and bromazolam itself. The typical dosage range for bromazolam is between 1 to 2 mg, although effects may be observed at lower doses of 0.5 to 1.0 mg, with some individuals requiring higher doses of up to 2 to 4 mg.

Metabolism and Duration of Action

Bromazolam is primarily metabolized in the liver through the cytochrome P450 (CYP450) enzyme complex, particularly by the CYP3A4 enzyme. Following oral intake, bromazolam exhibits an onset of action ranging from 15 to 45 minutes. The duration of its effects typically lasts between 5 to 8 hours, with after-effects potentially persisting for an additional 1 to 12 hours.

Mechanism of Action

The pharmacological effects of bromazolam are primarily mediated through the modulation of gamma-aminobutyric acid (GABA), the principal inhibitory neurotransmitter in the central nervous system (CNS). GABA exerts its effects by binding to GABA receptors located on neuronal membranes, initiating a cascade of events that lead to neuronal inhibition. There are three known types of GABA receptors: A, B, and C, with GABA-A receptors being ligand-gated chloride ion channels composed of five subunits: one γ subunit, two β subunits, and two α subunits.

When GABA binds to GABA-A receptors, it causes the opening of chloride ion channels, resulting in an influx of chloride ions into the neuron. This influx induces hyperpolarization of the neuron, thereby decreasing neuronal excitability. Benzodiazepines, including bromazolam, bind to a specific site located between the γ and α subunits of GABA-A receptors. This binding induces a conformational change in the receptor, enhancing its affinity for GABA and amplifying its inhibitory effects.

Affinity and Effects

The pharmacological response to bromazolam includes sedation, anxiolysis, hypnosis, skeletal muscle relaxation, and anticonvulsant activity. The GABA-A receptor has several subtypes, and different benzodiazepines exhibit varying affinities for these subtypes, leading to diverse effects. Bromazolam, in particular, has a notable affinity for the α1, α2, and α5 subtypes of the GABA-A receptor, which contributes to its sedative and anxiolytic properties.

Conclusion

While bromazolam has not been approved for medical use, its unique pharmacological profile and potential effects make it a subject of interest in research settings. Understanding its mechanism of action, metabolism, and effects is essential for further exploration of its therapeutic potential and safety profile. As with any psychoactive substance, caution is advised, and further studies are necessary to fully elucidate the implications of bromazolam use.

Bromazolam 4mg Pellets is for research use only and not intended for human consumption!

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Bromazolam 4mg Pellets stock last updated at: April 2025