Drug intelligence / Profile preview

clonazolam

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral, Sublingual, Intranasal, Inhalation
01

Overview

Clonazolam is a potent triazolobenzodiazepine (TBZD), a subclass of benzodiazepines characterized by the fusion of a triazole ring to the benzodiazepine structure. First synthesized in 1971, it was found to be the most active compound among its analogues but has never been licensed for therapeutic use. Clonazolam acts as a central nervous system depressant and is sold online as a designer drug or research chemical. Its primary mechanism involves allosteric potentiation of gamma-aminobutyric acid (GABA) activity at GABAA receptors, leading to increased chloride ion influx and neuronal inhibition. This results in effects such as strong sedation, muscle relaxation, amnesia, loss of motor control, respiratory depression, and high dependence liability even at very low doses (as small as 0.5 mg). Clonazolam is structurally related to clonazepam but exhibits higher potency and risk profile[1][2][3][7][8].

Other names
clonitrazolam
02

Targets

GABRR (GABA-A receptor subunit rho)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)GABRA3 (Gamma-aminobutyric acid receptor subunit alpha-3)GABRA5 (Gamma-aminobutyric acid type A receptor subunit alpha-5)

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