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MK-801可逆转全多巴胺D1受体激动剂SKF-82958在大鼠纹状体中诱导的Fos表达。

MK-801 reverses Fos expression induced by the full dopamine D1 receptor agonist SKF-82958 in the rat striatum.

作者信息

Nakazato E, Ohno M, Watanabe S

机构信息

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.

出版信息

Eur J Pharmacol. 1998 Jan 26;342(2-3):209-12. doi: 10.1016/s0014-2999(97)01571-9.

DOI:10.1016/s0014-2999(97)01571-9
PMID:9548387
Abstract

Administration of the selective and full dopamine D1 receptor agonist SKF-82958 ((+/-)-6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-b enzazepine) (1 and 3 mg/kg i.p.) led to a dose-dependent induction of Fos protein in the rat striatum. The 3 mg/kg SKF-82958-induced expression of striatal Fos protein was blocked by the dopamine D1 receptor antagonist SCH-23390 (R(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benza zepine) (0.3 mg/kg i.p.). The noncompetitive NMDA receptor antagonist MK-801 ((5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]-cyclohepten-5 ,10-imine) (1 mg/kg i.p.) also completely prevented striatal Fos induction by an injection of 3 mg/kg SKF-82958. These results suggest that dopamine D1 receptor activation by the full agonist SKF-82958 is sufficient to trigger Fos expression in the striatum, but that concomitant stimulation of NMDA receptors is required for the striatal Fos induction in response to dopamine D1 receptor activation.

摘要

给予选择性且完全的多巴胺D1受体激动剂SKF - 82958((±)-6 - 氯 - 7,8 - 二羟基 - 3 - 烯丙基 - 1 - 苯基 - 2,3,4,5 - 四氢 - 1H - 3 - 苯并氮杂卓)(腹腔注射1和3毫克/千克)导致大鼠纹状体中Fos蛋白呈剂量依赖性诱导。腹腔注射0.3毫克/千克的多巴胺D1受体拮抗剂SCH - 23390(R(+)-7 - 氯 - 8 - 羟基 - 3 - 甲基 - 1 - 苯基 - 2,3,4,5 - 四氢 - 1H - 3 - 苯并氮杂卓)可阻断3毫克/千克SKF - 82958诱导的纹状体Fos蛋白表达。非竞争性N - 甲基 - D - 天冬氨酸(NMDA)受体拮抗剂MK - 801((5R,10S)-(+)-5 - 甲基 - 10,11 - 二氢 - 5H - 二苯并[a,d] - 环庚烯 - 5,10 - 亚胺)(腹腔注射1毫克/千克)也完全阻止了注射3毫克/千克SKF - 82958后纹状体Fos的诱导。这些结果表明,完全激动剂SKF - 82958激活多巴胺D1受体足以触发纹状体中的Fos表达,但响应多巴胺D1受体激活时,纹状体Fos诱导需要同时刺激NMDA受体。

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