Zhang X, Nakata Y, Kikuchi T, Segawa T
Department of Pharmacology, Hiroshima University School of Medicine, Japan.
Pharm Res. 1990 Mar;7(3):280-2. doi: 10.1023/a:1015882314302.
7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D-2 receptor antagonist (Yasuda et al., Life Sci. 42: 1941-1954, 1988), was studied for its binding characteristics at 3H-SCH 23390-labeled dopamine D-1 receptors and 3H-spiperone-labeled dopamine D-2 receptors in rat striatum. The binding affinity of OPC-4392 for 3H-spiperone-labeled D-2 receptors was 500 times higher than for 3H-SCH 23390-labeled D-1 receptors. 6-Hydroxydopamine lesions of striatum and high-frequency current lesions of medial forebrain bundle did not affect the competition of OPC-4392 for 3H-spiperone binding. Kainic acid lesions of striatum significantly changed the one-site model fit to a two-site model fit of the competition curve of OPC-4392 for 3H-spiperone binding, suggesting that OPC-4392 competed with 3H-spiperone binding differently for postsynaptic dopamine D-2 receptors and for presynaptic dopamine autoreceptors.
7-[3-(4-[2,3-二甲基苯基]哌嗪基)丙氧基]-2(1H)-喹啉酮(OPC-4392)是一种突触前多巴胺自身受体激动剂和突触后D-2受体拮抗剂(Yasuda等人,《生命科学》42:1941 - 1954,1988),我们研究了它在大鼠纹状体中与3H-SCH 23390标记的多巴胺D-1受体和3H-螺哌隆标记的多巴胺D-2受体的结合特性。OPC-4392对3H-螺哌隆标记的D-2受体的结合亲和力比对3H-SCH 23390标记的D-1受体高500倍。纹状体的6-羟基多巴胺损伤和内侧前脑束的高频电流损伤不影响OPC-4392对3H-螺哌隆结合的竞争。纹状体的 kainic 酸损伤显著改变了OPC-4392对3H-螺哌隆结合竞争曲线的单位点模型拟合为双位点模型拟合,表明OPC-4392与3H-螺哌隆结合对突触后多巴胺D-2受体和突触前多巴胺自身受体的竞争方式不同。