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麦角衍生物的多巴胺模拟活性,通过兔离体视网膜中环磷酸腺苷的生成来测定。

Dopamine-mimetic activity of ergot derivatives, as measured by the production of cyclic AMP in isolated retinae of the rabbit.

作者信息

Schorderet M

出版信息

Gerontology. 1978;24 Suppl 1:86-93. doi: 10.1159/000212302.

Abstract

The effects of several ergot alkaloid derivatives on the concentration of cyclic AMP in intact rabbit retinae were investigated in vitro. All compounds were found to be potent inducers of cyclic AMP production, half-maximal stimulation being obtained at 10(-6)M, and maximal stimulation at 10(-4)M concentrations. The range of effective concentrations was very well comparable with that of dopamine (or apomorphine) in the same experimental conditions. Furthermore, the accumulation of cyclic AMP induced by the ergot derivatives was blocked by fluphenazine, at 10(-4)-5 X 10(-4)M, or lithium, at 5 X 10(-2)M concentrations. Both antipsychotic drugs were found to be very potent inhibitors of dopamine-(or apomorphine-) induced production of cyclic AMP in the same preparation. A potential dopamine-mimetic activity of ergot derivatives (or of other dopamine-like drugs) can be specifically tested on isolated rabbit retinae in vitro, either before undertaking experiments in vivo or in correlation with behavioural studies.

摘要

在体外研究了几种麦角生物碱衍生物对完整兔视网膜中环磷酸腺苷(cAMP)浓度的影响。发现所有化合物都是cAMP产生的有效诱导剂,在10^(-6)M浓度时获得半数最大刺激,在10^(-4)M浓度时获得最大刺激。在相同实验条件下,有效浓度范围与多巴胺(或阿扑吗啡)的非常相似。此外,在10^(-4) - 5×10^(-4)M浓度的氟奋乃静或5×10^(-2)M浓度的锂可阻断麦角衍生物诱导的cAMP积累。在同一制剂中,发现这两种抗精神病药物都是多巴胺(或阿扑吗啡)诱导的cAMP产生的非常有效的抑制剂。在进行体内实验之前或与行为研究相关联时,可以在体外分离的兔视网膜上专门测试麦角衍生物(或其他多巴胺样药物)的潜在多巴胺模拟活性。

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