Selective D2 dopamine receptor agonists prevent catalepsy induced by SCH 23390, a selective D1 antagonist.

Selective D2 dopamine receptor agonists prevent catalepsy induced by SCH 23390, a selective D1 antagonist.
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选择性 D2 多巴胺受体激动剂可预防由选择性 D1 拮抗剂 SCH 23390 引起的僵直症。

DOI:
10.1016/0024-3205(85)90159-6
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发表时间:
1985
期刊:
影响因子:
6.1
通讯作者:
Goldstein,M
Goldstein,M
中科院分区:
医学2区
文献类型:
--
作者:
Meller,E;Kuga,S;Friedhoff,AJ;Goldstein,M

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SCH 23390是一种中枢D1多巴胺受体的明显选择性拮抗剂,在低剂量(0.1 mg/kg,sc)下可引起严重僵住。用选择性D 2受体激动剂LY 141865、RU 24213或LY 171555(LY 141865的活性(-)对映体)预处理,引起对僵硬反应的剂量依赖性抑制。培高利特和阿扑吗啡也有效。该效应不是由于SCH 23390的分布改变或渗透入脑所致,因为完全阻断僵住症的LY 171555预处理对SCH 23390抑制离体测定的3 H-顺式-piflutixol与D 1受体结合的ID 50无影响。替代机制被认为是解释的结果,这提供了新的见解纹状体多巴胺能调节运动活动。
SCH 23390, an apparently selective antagonist of central D 1 dopamine receptors, produced profound catalepsy at low doses (0.1 mg/kg, sc). Pretreatment with the selective D 2 receptor agonists LY 141865, RU 24213 or LY 171555, the active (−) enantiomer of LY 141865, elicited a dose-dependent inhibition of the cataleptic response. Pergolide and apomorphine were also effective. This effect was not due to altered disposition or penetration of SCH 23390 into the brain since pretreatment with a dose of LY 171555 which completely blocked catalepsy had no effect on the ID 50 of SCH 23390 to inhibit 3 H-cis-piflutixol binding to D 1 receptors measured ex vivo. Alternative mechanisms are considered to explain the results, which offer new insights into striatal dopaminergic regulation of motor activity.
DOI: --
发表时间: 1983-08
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
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