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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Dopamine D1/D2 antagonist combinations as antagonists of the discriminative stimulus effects of cocaine.
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Dopamine D1/D2 antagonist combinations as antagonists of the discriminative stimulus effects of cocaine.

机译：多巴胺D1 / D2拮抗剂组合可卡因的歧视性刺激作用的拮抗剂。

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Although data suggest that the dopaminergic system mediates the discriminative stimulus effects of cocaine, neither selective D1 or D2 dopamine agonists nor selective D1 or D2 antagonists substitute reliably for or consistently block these effects. These findings suggest that concurrent activity at these receptor subtypes may underlie this discrimination. Accordingly, it would be expected that simultaneous blockade of these receptors may be necessary to block it fully. The ability of various combinations of the D1 antagonist, SCH 23,390, and the D2 antagonist, haloperidol, were tested for their ability to block the cocaine stimulus in rats trained to discriminate cocaine (7.5, 10, or 13 mg/kg) from vehicle. Antagonist combinations decreased the percentage of cocaine-appropriate responses 10-95% below the cocaine baseline at doses of the antagonist that were inactive when given separately. These findings support the position that activity at D1-like and D2-like receptor subtypes may account for more of the pharmacological action of cocaine than activation of a single dopamine receptor subtype.
机译：尽管数据表明多巴胺能系统介导了可卡因的歧视性刺激作用，但选择性D1或D2多巴胺激动剂和选择性D1或D2拮抗剂均不能可靠地替代或始终阻断这些作用。这些发现表明，在这些受体亚型上的同时活性可能是这种区分的基础。因此，预期可能需要同时阻断这些受体才能完全阻断它。测试了D1拮抗剂SCH 23,390和D2拮抗剂氟哌啶醇各种组合的阻断阻断可卡因刺激的能力，这些大鼠经训练可从媒介物中区分可卡因（7.5、10或13 mg / kg）。拮抗剂组合使可卡因适当的反应百分比在可单独使用时无活性的拮抗剂剂量下比可卡因基线降低了10-95％。这些发现支持了这样的观点，即与单一多巴胺受体亚型的激活相比，对D1类和D2类受体亚型的活性可解释可卡因的更多药理作用。

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