Ro5-4864

Ro5-4864 (4'-chlorodiazepam) is a benzodiazepine derivative that acts as a selective ligand for the 18 kDa translocator protein (TSPO), formerly known as the peripheral benzodiazepine receptor (PBR). Unlike traditional benzodiazepines, Ro5-4864 has negligible affinity for the central GABA-A receptor complex but binds with high affinity to TSPO located on the outer mitochondrial membrane. It is extensively utilized as a pharmacological research tool to investigate the role of TSPO in cholesterol transport, neurosteroidogenesis, apoptosis, and inflammation. Recent studies have demonstrated that Ro5-4864 can induce relaxation in airway smooth muscle (ASM) by modulating intracellular calcium flux and reducing the phosphorylation of myosin light chain 20 (pMLC20), suggesting potential therapeutic applications in obstructive airway diseases such as asthma.

Other names

4'-chlorodiazepam4-chlorodiazepam7-chloro-5-(4-chlorophenyl)-1-methyl-3H-1,4-benzodiazepin-2-one