Skarsfeldt T
Department of Pharmacology, H. Lundbeck A/S, Copenhagen, Valby, Denmark.
Eur J Pharmacol. 1988 Jan 12;145(2):239-43. doi: 10.1016/0014-2999(88)90238-5.
The effect of chronic treatment (21 days s.c.) with SCH 23390 and haloperidol on spontaneously active DA neurones in substantia nigra pars compacta (SNC) and ventral tegmental area (VTA) was studied in rats by means of single unit recording techniques. The specific DA D-1 receptor antagonist SCH 23390 was injected twice daily in one of the following doses: 0.06, 0.23, 0.46 or 0.90 mumol/kg. SCH 23390 decreased the number of spontaneously active neurones in SNC and VTA to the same extent. The DA D-2 receptor antagonist haloperidol was injected once daily in one of the following doses: 0.05, 0.21 or 1.7 mumol/kg and induced a decrease in the number of spontaneously active DA neurones in SNC and VTA. These results suggest that SCH 23390 has a profile similar to that of haloperidol and that SCH 23390 has clinical antipsychotic activity but also induces extrapyramidal side-effects.
采用单单位记录技术，在大鼠中研究了SCH 23390和氟哌啶醇慢性治疗（皮下注射21天）对黑质致密部（SNC）和腹侧被盖区（VTA）中自发活动的多巴胺能神经元的影响。特异性多巴胺D-1受体拮抗剂SCH 23390每天注射两次，剂量如下：0.06、0.23、0.46或0.90 μmol/kg。SCH 23390使SNC和VTA中自发活动神经元的数量减少程度相同。多巴胺D-2受体拮抗剂氟哌啶醇每天注射一次，剂量如下：0.05、0.21或1.7 μmol/kg，并导致SNC和VTA中自发活动的多巴胺能神经元数量减少。这些结果表明，SCH 23390具有与氟哌啶醇相似的作用模式，且SCH 23390具有临床抗精神病活性，但也会诱发锥体外系副作用。
