Protais P, Hermier C, Costentin J
Neuropharmacology. 1985 Sep;24(9):861-7. doi: 10.1016/0028-3908(85)90037-1.
The cataleptogenic effect or the antagonism of apormorphine-induced behaviour (climbing, sniffing, licking and yawning) shown by haloperidol, (+/-)sulpiride and (+/-)amisulpride were determined at different times after their intraperitoneal or intraventricular administration. After intraperitoneal injection, the ED50 or ID50 of haloperidol was similar for all the behavioural responses. On the other hand, sulpiride and amisulpride were effective on climbing and yawning in smaller doses than on sniffing, licking and catalepsy. The property of amisulpride to antagonize climbing at smaller doses than sniffing was still found whether this benzamide derivative was injected 30, 90, 150 or 240 min before testing. After the intraventricular administration of neuroleptics, a dissociated antagonist efficacy appeared for haloperidol, but that of sulpiride and amisulpride became much more marked than after their intraperitoneal injection. Amisulpride antagonized climbing in smaller doses than sniffing, whether administered intraventricularly 15, 30 or 120 min before testing. These results indicate that the dissociated dopamine antagonist efficacy of benzamides is long lasting and is observed even when the passage across the blood-brain barrier is avoided (i.c.v. route).
在腹腔注射或脑室内注射氟哌啶醇、（±）舒必利和（±）阿立哌唑后不同时间，测定了它们的致僵作用或对阿扑吗啡诱导行为（攀爬、嗅闻、舔舐和打哈欠）的拮抗作用。腹腔注射后，氟哌啶醇对所有行为反应的半数有效剂量（ED50）或半数抑制剂量（ID50）相似。另一方面，舒必利和阿立哌唑对攀爬和打哈欠的有效剂量比对嗅闻、舔舐和致僵的有效剂量小。无论在测试前30、90、150或240分钟注射这种苯甲酰胺衍生物，阿立哌唑在比嗅闻更小的剂量下拮抗攀爬的特性仍然存在。在脑室内注射抗精神病药物后，氟哌啶醇出现了分离的拮抗作用，但舒必利和阿立哌唑的拮抗作用比腹腔注射后更为明显。无论在测试前15、30或120分钟脑室内注射，阿立哌唑在比嗅闻更小的剂量下拮抗攀爬。这些结果表明，苯甲酰胺类药物的分离多巴胺拮抗作用是持久的，即使避免穿过血脑屏障（脑室内途径）也能观察到。
