Drug intelligence / Profile preview

bromazolam

Development stage
Discontinued
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Bromazolam is a synthetic triazolobenzodiazepine, first synthesized in 1976 but never marketed as a medicinal drug. It is structurally related to alprazolam, differing by the substitution of a bromo group for chloro. Bromazolam acts as a non-selective positive allosteric modulator at the benzodiazepine site of the gamma-aminobutyric acid type A (GABAA) receptor complex, binding with high affinity to α1, α2, and α5 subunits. Its pharmacological effects are similar to other benzodiazepines and include sedation, anxiolysis, muscle relaxation, anticonvulsant activity, and amnesia. Bromazolam has been sold online as a designer drug since its first detection in Sweden in 2016 and has appeared on illicit markets often misrepresented as legal benzodiazepines such as alprazolam or diazepam. It is not approved for medical use anywhere but is controlled under various national regulations due to concerns about misuse and associated fatalities—especially when combined with opioids like fentanyl[3][5][7].

Other names
bromazolamXLI-268XLI268XLI 268
02

Targets

GABRR (GABA-A receptor subunit rho)

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