Zetler G
Neuropharmacology. 1986 Nov;25(11):1213-20. doi: 10.1016/0028-3908(86)90138-3.
Compulsive gnawing was produced in mice by administration of either methylphenidate or (after sensitizing pretreatment with the neuroleptic, tetflutixol) apomorphine. Drugs which antagonise stereotypy, such as ceruletide (CER, a sulphated decapeptide related to cholecystokinin octapeptide), haloperidol, zuclopenthixol and fluphenazine were applied in equipotent doses (reducing stereotypy by 80%). Clonazepam, muscimol, clonidine and scopolamine (but not methylscopolamine) antagonized to a different extent the antistereotype effect of ceruletide and the neuroleptics. The ED50s for clonazepam and other drugs, were determined; clonazepam had the greatest potency. Regarding the antagonism of the antistereotype effect, ceruletide was similar to but by no means congruent with haloperidol. The antagonism of the antistereotype effect was specific because other effects of ceruletide and cholecystokinin octapeptide (inhibition of exploratory rearing activity, ptosis, antinociception, hypothermia) were not antagonized by clonazepam and only weakly modified by scopolamine. Methylscopolamine was ineffective throughout, indicating a central site for the mechanism of the actions studied of scopolamine. In conclusion, the antistereotype effect of ceruletide is different from that of conventional neuroleptic drugs and functionally independent of other behavioural effects of the cholecystokinin-like peptides.
通过给予哌醋甲酯或（在用抗精神病药三氟噻吨进行致敏预处理后）阿扑吗啡，在小鼠中产生强迫性啃咬行为。使用了能拮抗刻板行为的药物，如蛙皮素（CER，一种与八肽胆囊收缩素相关的硫酸化十肽）、氟哌啶醇、珠氯噻醇和氟奋乃静，它们的剂量等效（可使刻板行为减少80%）。氯硝西泮、蝇蕈醇、可乐定和东莨菪碱（但不是甲基东莨菪碱）在不同程度上拮抗了蛙皮素和抗精神病药的抗刻板效应。测定了氯硝西泮和其他药物的半数有效剂量（ED50）；氯硝西泮的效力最强。关于抗刻板效应的拮抗作用，蛙皮素与氟哌啶醇相似但并不完全相同。抗刻板效应的拮抗作用具有特异性，因为蛙皮素和八肽胆囊收缩素的其他效应（抑制探索性竖毛活动、眼睑下垂、抗伤害感受、体温过低）并未被氯硝西泮拮抗，仅被东莨菪碱轻微改变。甲基东莨菪碱始终无效，表明东莨菪碱所研究作用机制的位点在中枢。总之，蛙皮素的抗刻板效应与传统抗精神病药物不同，并且在功能上独立于胆囊收缩素样肽的其他行为效应。
