Janssen P A, Niemegeers C J, Schellekens K H, Lenaerts F M, Wauquier A
Arzneimittelforschung. 1975 Aug;25(8):1287-94.
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 of diphenylbutylpiperidine neuroleptics of which pimozide is the prototype, In animals the pharmacological profile of R 29 764 resembles that of typical neuroleptic compounds. R29 764 is very potent by oral route and has an extremely long duration of action. The onset of action of clopimozide is relatively fast, it is already very potent after 4 h and, in the procedures described, reaches its peak effect 24 h after administration. In spite of the high potency and long duration of action clopimozide is relatively atoxic. The safety margin, calculated as the ratio between the acute LD50 value and the lowest ED50 value is larger than or equal to 15.000 in rats and greater than 7.250 in dogs. Qualitatively, R 29 764 is more closely related to haloperidol, pimozide and penfluridol than to chlorpromazine. The side effect liability is expected to be very low, when hypotensive, autonomic and undesirable neurological side effects are concerned.
氯哌莫齐（R 29 764），即5-氯-1-（4-[4,4-双（对氟苯基）丁基]-4-哌啶基）-2-苯并咪唑啉酮，是强效长效二苯基丁基哌啶类抗精神病药系列的新成员，以匹莫齐特为原型。在动物体内，R 29 764的药理特性类似于典型的抗精神病化合物。R29 764口服效力很强，作用持续时间极长。氯哌莫齐的起效相对较快，给药4小时后就已经效力很强，在所描述的实验过程中，给药后24小时达到最大效应。尽管氯哌莫齐效力高且作用持续时间长，但毒性相对较低。以急性半数致死量（LD50）值与最低半数有效量（ED50）值之比计算的安全系数，在大鼠中大于或等于15000，在犬中大于7250。从性质上讲，R 29 764与氟哌啶醇、匹莫齐特和五氟利多的关系比与氯丙嗪更为密切。就低血压、自主神经及不良神经副作用而言，预计其副作用发生率会非常低。
