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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Psychopharmacological distinction between novel full-efficacy 'D1-like' dopamine receptor agonists.
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Psychopharmacological distinction between novel full-efficacy 'D1-like' dopamine receptor agonists.

机译：新型全效“ D1样”多巴胺受体激动剂之间的心理药理学区别。

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The search for full-efficacy agonists selective for the "D1-like" family of dopamine receptor subtypes has recently generated two novel series of compounds: the isochromans, typified by A 68930, and the phenanthridines, typified by dihydrexidine. This study was undertaken to compare systematically the effects of these two agents on the spectrum of unconditioned motor behaviour (i.e., construction of their drug ethograms) in the intact adult rat and to determine the sensitivity of these responses to selective antagonists of "D1-like" (SCH 23390) vs. "D2-like" (YM 09151-2) receptors. A 68930 (0.0625-4.0 mg/kg) readily induced grooming, including intense grooming, the most widely accepted behavioural model of "D1-like" receptor stimulation; it also induced vacuous chewing, a more controversial model thereof, and sniffing. Conversely, dihydrexidine (0.25-16.0 mg/kg) induced grooming, but little intense grooming was evident; it failed to induce vacuous chewing but did induce sniffing. Grooming and sniffing responses to A 68930 were readily blocked by SCH 23390 (0.01-1.0 mg/kg) but were only attenuated or spared by YM 09151-2 (0.005-0.5 mg/kg). Conversely, the grooming and sniffing responses to dihydrexidine were readily blocked both by SCH 23390 and by YM 09151-2. A 68930 and dihydrexidine do not show identical psychopharmacological profiles; they appear to differ in the specificity of their effects on "D1-like" vs. "D2-like" function and may interact differentially with putative subtypes of "D1-like" receptors that are indicated behaviourally.
机译：寻找对多巴胺受体亚型的“ D1样”家族有选择性的全效激动剂的研究最近产生了两种新型化合物：以A 68930为代表的异色团和以二氢己啶为代表的菲啶。进行这项研究的目的是系统地比较这两种药物对完整成年大鼠无条件运动行为谱的影响（即，构建其药物表），并确定这些反应对“ D1样”选择性拮抗剂的敏感性（SCH 23390）与“ D2类”（YM 09151-2）受体进行比较。 68930（0.0625-4.0 mg / kg）易于诱导修饰，包括强力修饰，这是最广泛接受的“ D1样”受体刺激行为模型;它也引起了空泡的咀嚼，一种更具争议的模型，以及嗅闻。相反，二氢己定（0.25-16.0 mg / kg）诱导修饰，但几乎没有明显的修饰。它不能引起空泡的咀嚼，但是可以引起嗅觉。 SCH 23390（0.01-1.0 mg / kg）可以轻松阻断对A 68930的修饰和嗅探反应，但YM 09151-2（0.005-0.5 mg / kg）只能减弱或避免其修饰。相反，SCH 23390和YM 09151-2都容易阻止对二氢己定的修饰和嗅探反应。 68930和二氢己定没有显示出相同的心理药理学特征;它们似乎对“ D1样”和“ D2样”功能的作用特异性不同，并且可能与行为上表明的推定的“ D1样”受体亚型相互作用。

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