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D1受体激动剂SKF 38393对阿扑吗啡在大鼠中某些行为效应的影响。

Effect of the D1 receptor agonist SKF 38393 on some behavioural effects of apomorphine in rats.

作者信息

Zarkovsky A M, Cereska K S

机构信息

Department of Pharmacology, Tartu State University, Estonian SSR, USSR.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1989 Apr;339(4):383-6. doi: 10.1007/BF00736051.

Abstract

The dopamine receptor agonist apomorphine in experiments on rats in low doses (0.025-0.2 mg/kg, s.c.) induced yawning which reflected a selective activation of presynaptic dopamine receptors. In high doses (0.25-1.0 mg/kg) apomorphine induced stereotyped sniffing and yawning in consequence of postsynaptic D2 receptor activation. Dopamine D1 receptor agonist SKF 38393 inhibited yawning induced by low doses of apomorphine. The inhibitory effect of SKF 38393 on apomorphine-induced yawning was attenuated by pretreatment with specific D1 receptor antagonist SCH 23390 [2-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol). On the other hand however, SKF 38393 potentiated sniffing induced by the high doses of apomorphine without affecting gnawing. These data indicate that D1 receptor activation modulates both pre- and postsynaptic effects of apomorphine in opposite directions.

摘要

在对大鼠进行的实验中,低剂量(0.025 - 0.2毫克/千克,皮下注射)的多巴胺受体激动剂阿扑吗啡会诱发打哈欠,这反映了突触前多巴胺受体的选择性激活。高剂量(0.25 - 1.0毫克/千克)的阿扑吗啡会因突触后D2受体激活而诱发刻板的嗅探和打哈欠。多巴胺D1受体激动剂SKF 38393可抑制低剂量阿扑吗啡诱发的打哈欠。用特异性D1受体拮抗剂SCH 23390 [2-(+)-8-氯-2,3,4,5-四氢-3-甲基-5-苯基-1H-3-苯并氮杂卓-7-醇]预处理后,SKF 38393对阿扑吗啡诱发打哈欠的抑制作用减弱。然而,另一方面,SKF 38393增强了高剂量阿扑吗啡诱发的嗅探,而不影响啃咬。这些数据表明,D1受体激活以相反的方向调节阿扑吗啡的突触前和突触后效应。

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