Arnt J, Hyttel J
Psychopharmacology (Berl). 1985;85(3):346-52. doi: 10.1007/BF00428200.
The antagonistic effect of dopamine (DA) D-1 and D-2 antagonists against circling behaviour induced by various DA agonists in 6-OHDA-lesioned rats has been investigated. DA D-1/D-2 selectivity of agonists in vitro was measured by the stimulatory effect on DA-sensitive adenylate cyclase in rat striatal homogenates (D-1), the inhibitory effect on electrically-induced release of 3H-DA in rabbit striatal slices (D-2) and the affinity to 3H-piflutixol (D-1) and 3H-spiroperidol (D-2) binding sites in rat striatal membranes. The contralateral circling behaviour induced by the DA D-1 agonist SK & F 38393 was blocked by the DA D-1 antagonist, SCH 23390, and by the mixed DA D-1/D-2 antagonist cis(Z)-flupentixol, but was not influenced by the DA D-2 antagonists spiroperidol and clebopride. In contrast, circling behaviour induced by the preferential DA D-2 agonists pergolide and LY 171555 was blocked by clebopride, spiroperidol, and cis(Z)-flupentixol, but weakly or not influenced by SCH 23390. Apomorphine-induced circling behaviour was blocked by cis(Z)-flupentixol, partially antagonized by SCH 23390 and clebopride but not inhibited by spiroperidol, although the time-course of circling was changed. Combinations of SCH 23390 with spiroperidol or clebopride in low doses completely blocked the effect of apomorphine. These results indicate that DA D-1 and D-2 receptors mediate circling behaviour through separate mechanisms which can be independently manipulated with respective agonists and antagonists.(ABSTRACT TRUNCATED AT 250 WORDS)
研究了多巴胺(DA)D-1和D-2拮抗剂对6-羟基多巴胺(6-OHDA)损伤大鼠中各种DA激动剂诱导的转圈行为的拮抗作用。通过对大鼠纹状体匀浆中DA敏感的腺苷酸环化酶的刺激作用(D-1)、对兔纹状体切片中电诱导的3H-DA释放的抑制作用(D-2)以及对大鼠纹状体膜中3H-匹莫齐特(D-1)和3H-螺哌啶醇(D-2)结合位点的亲和力,测定了激动剂在体外的DA D-1/D-2选择性。DA D-1激动剂SK&F 38393诱导的对侧转圈行为被DA D-1拮抗剂SCH 23390和混合的DA D-1/D-2拮抗剂顺式(Z)-氟哌噻吨阻断,但不受DA D-2拮抗剂螺哌啶醇和氯氮平的影响。相反,优先的DA D-2激动剂培高利特和LY 171555诱导的转圈行为被氯氮平、螺哌啶醇和顺式(Z)-氟哌噻吨阻断,但受SCH 23390的影响较弱或不受影响。阿扑吗啡诱导的转圈行为被顺式(Z)-氟哌噻吨阻断,被SCH 23390和氯氮平部分拮抗,但不受螺哌啶醇抑制,尽管转圈的时间进程发生了变化。低剂量的SCH 23390与螺哌啶醇或氯氮平联合使用完全阻断了阿扑吗啡的作用。这些结果表明,DA D-1和D-2受体通过不同机制介导转圈行为,这些机制可分别用各自的激动剂和拮抗剂进行独立调控。(摘要截短于250字)