Puech A J, Simon P, Boissier J R
Eur J Pharmacol. 1978 Aug 15;50(4):291-300. doi: 10.1016/0014-2999(78)90134-6.
The effects of 6 benzamides and 8 classical neuroleptics were studied on 6 different apomorphine-induced effects. These drugs did not antagonize all the effects in the same way. The differences are discussed according to the two types of dopaminergic receptor hypothesis. Some apomorphine-induced effects (stereotyped behavior, circling behavior, climbing behavior, and increased motor activity) could be related to stimulation of one type of dopaminergic receptor, other effects (hypothermia and decreased activity) to the other type. Pimozide, sulpiride, thioproperazine, GRI 1665 and TER 1546, could block selectively one type of dopaminergic receptor, at least in a given range of doses. Clozapine, chlorpromazine, levomepromazine, and thioridazine, could block selectively the other type of dopaminergic receptor. Haloperidol, metoclopramide, prochlorperazine, sultopride, and tiapride, could block both types of dopaminergic receptors with equal intensity whatever the dose.
研究了6种苯甲酰胺类药物和8种经典抗精神病药物对6种不同阿扑吗啡诱导效应的影响。这些药物对所有效应的拮抗方式并不相同。根据两种多巴胺能受体假说对这些差异进行了讨论。一些阿扑吗啡诱导的效应(刻板行为、转圈行为、攀爬行为和运动活性增加)可能与一种多巴胺能受体的刺激有关,而其他效应(体温过低和活性降低)则与另一种多巴胺能受体有关。匹莫齐特、舒必利、硫丙拉嗪、GRI 1665和TER 1546至少在给定剂量范围内可选择性阻断一种多巴胺能受体。氯氮平、氯丙嗪、左美丙嗪和硫利达嗪可选择性阻断另一种多巴胺能受体。无论剂量如何,氟哌啶醇、甲氧氯普胺、丙氯拉嗪、舒托必利和替阿普明均可同等强度地阻断两种多巴胺能受体。