Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the GABA antagonist flumazenil, although its effects are somewhat different. It is classified as a high-potency benzodiazepine due to its high affinity binding to benzodiazepine binding sites where it acts as a partial agonist. Its profile as a partial agonist and preclinical trial data suggests that it may have a reduced adverse effect profile. In particular bretazenil has been proposed to cause a less strong development of tolerance and withdrawal syndrome. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α1, α2, α3, α4, α5 and α6 subunit containing GABAA receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α1, α2, α3 and α5 GABAA benzodiazepine receptor complexes.
ברטזניל molecular structure diagram from the DrugsPRO substance library.
Classification
Chemical: Benzodiazepine
Psychoactive: Depressant
Effects
Sedation
Motor Impairment
Muscle Relaxation
Reduced Anxiety
Anxiety Suppression
Amnesia
Dulled Perception
Routes of Administration
No route information available yet.
Harm Reduction
Check interactions before mixing substances, pay attention to dose spacing and hydration, and treat all dosage guidance as approximate rather than guaranteed safe.
Sources
Substance data is aggregated from the following public harm-reduction and reference sources.
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Bretazenil - מדריך חומרים של DrugsPRO
Bretazenil: Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the GABA antagonist flumazenil, although its effects are somewhat different. It is classified as