Ro5-4864

Ro5-4864

Ro5-4864[1] (4'-Chlorodiazepam) is a drug which is a benzodiazepine derivative, the 4'-chloro derivative of diazepam. However unlike most benzodiazepine derivatives, Ro5-4864 lacks affinity for GABAA receptors and lacks typical benzodiazepine effects,[2] instead being sedative yet also convulsant and anxiogenic in effects.[3][4][5][6] Ro5-4864 was found to be a potent ligand for the "peripheral benzodiazepine receptor",[7] later renamed to mitochondrial translocator protein 18kDa (TSPO). Despite its convulsant effects, at lower doses Ro5-4864 has proved to be neuroprotective and has become widely used for research into the role of the TSPO protein in neurotoxicity,[8][9][10][11][12][13] as well as having analgesic [14] and possible antidepressant,[15] cardioprotective and anti-cancer effects.[16][17][18][19]

See also

  • Diclazepam (2'-Chlorodiazepam)
  • PK-11195

References