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同时激活 D1 多巴胺受体(SKF 38393)可揭示 B-HT 920 在小鼠体内的 D2 多巴胺能作用。

Concomitant D1 dopamine receptor activation (SKF 38393) unmasks D2 dopaminergic actions of B-HT 920 in mice.

作者信息

Verma A, Kulkarni S K

机构信息

Department of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

Indian J Exp Biol. 1991 Feb;29(2):123-6.

PMID:1831182
Abstract

The present study attempts to demonstrate D1/D2 dopamine (DA) receptor interactions during stereotyped behaviour in mice. B-HT 920 [2-amino-6-allyl-5, 6, 7, 8-tetrahydro-4H-thiazolo-(4, 5-d)-azepine] (0.05-1.0 mg/kg), a selective D2-DA agonist, induced mild per se stereotypy consisting mainly of sniffing and rearing responses. Apomorphine, a mixed D1/D2 agonist, also produced typical stereotypic response in mice. The stereotypic response of B-HT 920 was blocked by D2-DA antagonist, sulpiride (50 mg/kg). The effect of apomorphine was not influenced by co-treatment with SKF 38393. Simultaneous administration of B-HT 920 (0.1-0.5 mg/kg) with SKF 38393 (5 mg/kg), a selective D1-DA agonist, elicited dramatic increase in stereotyped behaviours in naive as well as in 24 hr reserpinised (2 mg/kg) mice. Co-treatment of apomorphine (0.5 mg/kg) with B-HT 920 (0.1, 0.25 mg/kg) also resulted in a clearly synergistic effect on stereotyped behaviour. These potentiated responses were reduced or blocked by haloperidol, a D2-DA antagonist. The data suggest that in presence of concomitant stimulation of D1-DA receptors. B-HT 920 exhibits full expression of postsynaptic D2-DA receptor mediated behavioural effects.

摘要

本研究试图证明小鼠刻板行为过程中D1/D2多巴胺(DA)受体的相互作用。B-HT 920 [2-氨基-6-烯丙基-5,6,7,8-四氢-4H-噻唑并-(4,5-d)-氮杂卓](0.05-1.0毫克/千克),一种选择性D2-DA激动剂,本身诱导轻微的刻板行为,主要由嗅探和竖毛反应组成。阿扑吗啡,一种D1/D2混合激动剂,也在小鼠中产生典型的刻板反应。B-HT 920的刻板反应被D2-DA拮抗剂舒必利(50毫克/千克)阻断。阿扑吗啡的作用不受与SKF 38393联合治疗的影响。将B-HT 920(0.1-0.5毫克/千克)与选择性D1-DA激动剂SKF 38393(5毫克/千克)同时给药,在未处理的以及24小时利血平化(2毫克/千克)的小鼠中引发刻板行为的显著增加。阿扑吗啡(0.5毫克/千克)与B-HT 920(0.1、0.25毫克/千克)联合治疗也对刻板行为产生明显的协同作用。这些增强的反应被D2-DA拮抗剂氟哌啶醇降低或阻断。数据表明,在D1-DA受体同时受到刺激的情况下,B-HT 920表现出突触后D2-DA受体介导的行为效应的充分表达。

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