Clopimozide (R 29 764), a new highly potent and orally long-acting neuroleptic of the diphenylbutylpiperidine series.

摘要: Clopimozide (R 29 764), 5-chloro-1-(4-[4,4-bis(p-fluorophenyl)butyl]-4-piperidyl)-2-benzimidazolinone, is a new member of the potent and long-acting series diphenylbutylpiperidine neuroleptics which pimozide prototype, In animals pharmacological profile R 764 resembles that typical neuroleptic compounds. R29 very by oral route has an extremely long duration action. The onset action clopimozide relatively fast, it already after 4 h and, in procedures described, reaches its peak effect 24 administration. spite high potency atoxic. safety margin, calculated as ratio between acute LD50 value lowest ED50 larger than or equal to 15.000 rats greater 7.250 dogs. Qualitatively, more closely related haloperidol, penfluridol chlorpromazine. side liability expected be low, when hypotensive, autonomic undesirable neurological effects are concerned.