Hong M, Jenner P, Marsden C D
Neuropharmacology. 1987 Feb-Mar;26(2-3):237-45. doi: 10.1016/0028-3908(87)90214-0.
The effects of the monoamine depleting drugs oxypertine, tetrabenazine and reserpine were compared with those of the dopamine receptor antagonists, chlorpromazine and trifluoperazine, on behavioural and biochemical indices of dopamine function in the brain. Oxypertine (0.625-20 mg/kg, i.p.), chlorpromazine (0.625-20 mg/kg i.p.) and trifluoperazine (0.0625-2.0 mg/kg i.p.), administered to rats 1 hr previously, inhibited stereotyped behaviour induced by both amphetamine (5.0 mg/kg i.p.) and apomorphine (1.0 mg/kg, s.c.) in a dose-dependent manner. Tetrabenazine (0.625-20 mg/kg i.p., 1 hr previously) inhibited stereotypy induced by amphetamine but not that induced by apomorphine. Reserpine (0.1 10 mg/kg i.p., 6 hr previously) did not inhibit, but in larger doses, tended to enhance the stereotyped responses to both amphetamine and apomorphine. Oxypertine (10 mg/kg, i.p., 1 hr previously), tetrabenazine (5 mg/kg i.p., 1 hr previously) and reserpine (2.5 mg/kg i.p., 6 hr previously) reduced the content of dopamine in the striatum but increased the concentrations of homovanillic acid (HVA) and 3,4-dihydroxyphenylacetic acid (DOPAC). Chlorpromazine (5 mg/kg i.p.) and trifluoperazine (0.5 mg/kg i.p.), given 1 hr previously, did not alter concentrations of dopamine in the striatum but increased those of HVA and DOPAC. Oxypertine, chlorpromazine and trifluoperazine weakly inhibited dopamine-stimulated adenylate cyclase in homogenates of the striatum in the rat. Tetrabenazine and reserpine had no effect. Similarly, trifluoperazine and chlorpromazine displaced the specific binding of [3H]piflutixol to membranes from the striatum. Oxypertine also was weakly effective, but tetrabenazine and reserpine were without effect. Trifluoperazine, chlorpromazine and oxypertine displaced specific binding of [3H]spiperone and [3H]N,n-propylnorapomorphine (NPA) to preparations of the striatum.(ABSTRACT TRUNCATED AT 250 WORDS)
将单胺耗竭药物奥昔哌汀、丁苯那嗪和利血平的作用与多巴胺受体拮抗剂氯丙嗪和三氟拉嗪的作用进行了比较,观察它们对大脑中多巴胺功能的行为和生化指标的影响。提前1小时给大鼠腹腔注射奥昔哌汀(0.625 - 20毫克/千克)、氯丙嗪(0.625 - 20毫克/千克腹腔注射)和三氟拉嗪(0.0625 - 2.0毫克/千克腹腔注射),它们以剂量依赖的方式抑制了由苯丙胺(5.0毫克/千克腹腔注射)和阿扑吗啡(1.0毫克/千克,皮下注射)诱导的刻板行为。提前1小时给大鼠腹腔注射丁苯那嗪(0.625 - 20毫克/千克)抑制了由苯丙胺诱导的刻板行为,但不抑制由阿扑吗啡诱导的刻板行为。提前6小时给大鼠腹腔注射利血平(0.1 - 10毫克/千克)没有抑制作用,但在较大剂量时,倾向于增强对苯丙胺和阿扑吗啡的刻板反应。提前1小时给大鼠腹腔注射奥昔哌汀(10毫克/千克)、提前1小时给大鼠腹腔注射丁苯那嗪(5毫克/千克)和提前6小时给大鼠腹腔注射利血平(2.5毫克/千克)降低了纹状体中多巴胺的含量,但增加了高香草酸(HVA)和3,4 - 二羟基苯乙酸(DOPAC)的浓度。提前1小时给大鼠腹腔注射氯丙嗪(5毫克/千克)和三氟拉嗪(0.5毫克/千克)没有改变纹状体中多巴胺的浓度,但增加了HVA和DOPAC的浓度。奥昔哌汀、氯丙嗪和三氟拉嗪在大鼠纹状体匀浆中对多巴胺刺激的腺苷酸环化酶有微弱抑制作用。丁苯那嗪和利血平没有作用。同样,三氟拉嗪和氯丙嗪能取代[³H]匹氟噻吨与纹状体膜的特异性结合。奥昔哌汀也有微弱作用,但丁苯那嗪和利血平没有作用。三氟拉嗪、氯丙嗪和奥昔哌汀能取代[³H]螺哌隆和[³H]N,N - 丙基去甲阿扑吗啡(NPA)与纹状体制剂的特异性结合。(摘要截短于250字)