Ro5-4864
Aliases: 4'-chlorodiazepam, 4-chlorodiazepam
Categories
Summary
4'-Chlorodiazepam (Ro5-4864) displays nanomolar affinity for the peripheral benzodiazepine receptor/TSPO located on the outer mitochondrial membrane while showing orders-of-magnitude lower affinity for central GABA-A sites. Low-dose TSPO activation can produce neurosteroidogenesis and mild sedation; higher micromolar concentrations become anxiogenic and pro-convulsant in animals. Median convulsive dose (CD₅₀) in mice approximately 42 mg/kg i.p. No controlled human pharmacokinetic data exist. Extrapolations from dog and rat studies suggest oral bioavailability approximately 40-60% and an elimination half-life of 6-9 hours, with no confirmed active metabolites.
Dose Information
| ROA | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| Oral BA 40-60% | - | - | - | 5+mg(markedseizureriskinanimals)+ |
Light
Common
Strong
Heavy
Onset, Duration & After-effects
| ROA | Onset | Peak | Offset | After Effects |
|---|---|---|---|---|
| Oral | 20-60 min | 1-3 hrs | 2-3 hrs | 12-24 hrs |
Tolerance
Build-up
develops over 1–4 weeks of daily use; hypnotic tolerance faster than anxiolytic tolerance
Reset
weeks to months depending on half-life and duration of use; taper recommended
Effects
Positive
- Muscle Relaxation
Negative
- Tremor
- Headache
- Motor impairment
- Mild Sedation
- Sedation
Positive
- Reduced anxiety
Negative
- Inner Restlessness
- Anxiety Enhancement
- Memory Suppression
- Derealisation
Positive
Negative
- Tinnitus
- Visual Distortion
- Dulled perception