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外周腺苷受体的亚类。

Subclasses of external adenosine receptors.

作者信息

Londos C, Cooper D M, Wolff J

出版信息

Proc Natl Acad Sci U S A. 1980 May;77(5):2551-4. doi: 10.1073/pnas.77.5.2551.

Abstract

Cell surface adenosine receptors mediate either stimulation or inhibition of adenylate cyclase activity [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1], and the receptors that mediate these different responses can be discriminated with selected adenosine analogs. 5'-N-Ethylcarboxamide-adenosine is a more potent agonist at stimulatory receptors (Ra) than is N6-phenylisopropyladenosine, whereas the reverse potency order is seen with inhibitory receptors (Ri). The potency of adenosine is intermediate between the potencies of these two analogs. The relative potencies of adenosine receptor agonists are maintained in physiological responses in intact cells, such as steroidogenesis and inhibition of lipolysis. As with adrenergic receptors, subclasses of adenosine receptors differ functionally and pharmacologically.

摘要

细胞表面腺苷受体介导腺苷酸环化酶活性[ATP焦磷酸裂解酶(环化),EC 4.6.1.1]的刺激或抑制,并且介导这些不同反应的受体可用选定的腺苷类似物加以区分。5'-N-乙基甲酰胺基腺苷作为激动剂对刺激性受体(Ra)的作用比N6-苯异丙基腺苷更强,而对于抑制性受体(Ri),效力顺序则相反。腺苷的效力介于这两种类似物之间。腺苷受体激动剂的相对效力在完整细胞的生理反应中得以保持,如类固醇生成和脂解抑制。与肾上腺素能受体一样,腺苷受体的亚类在功能和药理学上也有所不同。

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