Ro5-4864 - Substance Search

Summary TheDrug.Wiki TripSit

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.

Dose Information TheDrug.Wiki

ROA	Light	Common	Strong	Heavy
Oral BA 40-60%	-	-	-	5+mg(markedseizureriskinanimals)+

Light Common Strong Heavy

Onset, Duration & After-effects TheDrug.Wiki

ROA	Onset	Peak	Offset	After Effects
Oral	20-60 min	1-3 hrs	2-3 hrs	12-24 hrs

Effect Profile

Scores (1–10) curated from multiple sources:

Effect keyword matching from PsychonautWiki catalog
Weighted by importance: core (×3), major (×2), minor (×1)

Full methodology

Benzodiazepine 5.3

Moderate+ 5/10

Moderate sedation with mild anxiolysis, low cognitive impairment

Anxiolysis ×3

5

reduced anxiety muscle relaxation

Sedation / Relaxation ×2

7

sedation mild sedation muscle relaxation

⚠ Motor / Cognitive Impairment ×1

2

memory suppression

Euphoria / Mood Lift ×1

0

Based on reports from:

Erowid Experience Reports PsychonautWiki Ro5-4864

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

Tolerance Decay

Full tolerance 3d Half tolerance 7d Baseline ~14d

Rodent literature shows TSPO desensitization over several days of dosing, but human tolerance dynamics are unknown; treat as potentially habit‑forming with partial cross‑tolerance only to other TSPO ligands. Data quality is low and largely theoretical/anecdotal.