Library
Ro5-4864
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.
Also known as: 4'-chlorodiazepam, 4'-Chlordiazepam
Classification
- Chemical: Benzodiazepine
- Tag: Not psychoactive
- Tag: Research-Chemical
- Tag: Tentative
Effects
- Mild Sedation
- Muscle Relaxation
- Tremor
- Headache
- Sedation
- Restlessness
- Derealization
- Inner Restlessness
- Anxiety Enhancement
- Memory Suppression
- Depersonalization
- Memory Impairment
- Tinnitus
- Visual Distortion
- Ringing
- Blurred Vision
Routes of Administration
Oral
Dosage
- Threshold: 0.25 – 0.5 mg
- Light: 0.5 – 1.5 mg
- Common: 1.5 – 3 mg
- Strong: 3 – 5 mg
- Heavy: 5 mg + (significant seizure risk suggested by animal literature; human safety unknown)
Duration
- Onset: 0.33-1 h
- Peak: 1-3 h
- Offset: 2-3 h
- After Effects: 12-24 h
- Total Duration: 4-8 h
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.
Links
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