Markstein R, Gull P, Rüdeberg C, Urwyler S, Jaton A L, McAllister K, Dixon A K, Hoyer D
Sandoz Pharma Ltd., Basle, Switzerland.
J Neural Transm (Vienna). 1996;103(3):261-76. doi: 10.1007/BF01271238.
SDZ PSD 958, a novel benzo[g]quinoxaline derivative exhibits the properties of a potent orally active selective D1 receptor antagonist. It has high affinity for D1-like receptors (D1, D5; pKi = 9.7-9.8) labelled by [3H]SCH23390 and is at least 400 fold less active at D2-like receptors (i.e. D2, D4) labelled by [3H]spiperone. Effects in functional tests are consistent with D1 receptor antagonist properties. SDZ PSD 958 inhibited apomorphine-induced rearing in mice and prevented prolongation of novelty-induced locomotion in rats elicited by the selective D1 receptor agonist CY 208-243. By contrast, SDZ PSD 958 did not induce catalepsy and only weakly inhibited apomorphine-induced stereotyped gnawing in rats. This suggests that SDZ PSD 958 preferentially inhibits responses mediated by dopamine systems innervating the limbic system.
SDZ PSD 958是一种新型苯并[g]喹喔啉衍生物，具有强效口服活性选择性D1受体拮抗剂的特性。它对由[3H]SCH23390标记的D1样受体（D1、D5；pKi = 9.7 - 9.8）具有高亲和力，而对由[3H]螺哌隆标记的D2样受体（即D2、D4）的活性至少低400倍。功能测试中的效应与D1受体拮抗剂特性一致。SDZ PSD 958抑制了阿扑吗啡诱导的小鼠竖毛反应，并阻止了选择性D1受体激动剂CY 208 - 243引起的大鼠新奇诱导运动的延长。相比之下，SDZ PSD 958不会诱发僵住症，且仅微弱抑制阿扑吗啡诱导的大鼠刻板啃咬行为。这表明SDZ PSD 958优先抑制由支配边缘系统的多巴胺系统介导的反应。
