肾血管舒张dopexamine和fenoldopam由于α1-adrenoceptor封锁。

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马丁•SW Broadley KJ

肾血管舒张dopexamine和fenoldopam由于α1-adrenoceptor封锁。

Br杂志。1995;115 (2):349 - 55。

PubMed ID

7670737 (在PubMed

]

文摘

1。鼠模型包括肾脏的肾血管反应D1-receptor多巴胺受体激动剂,dopexamine和fenoldopam检查。2。原位灌注肾脏都是恒定流量(11毫升最低为1)Krebs-bicarbonate解决方案在37度c .灌注压力监控,使血管舒张反应来衡量,提出的休息灌注压力注入去甲肾上腺素(6 x 10(9)米)。3。剂量相关血管舒张反应剂量dopexamine和fenoldopam。然而,这些并不反感D1-receptor拮抗剂,原理图23390,表明D1-receptors没有涉及。4所示。丸α1-adrenoceptor拮抗剂的剂量,剂量相关血管舒张药哌唑嗪,造成类似的反应表明,α1-adrenoceptor dopexamine阻塞性质和fenoldopam负责血管舒张。5。alpha-Adrenoceptor封锁dopexamine和fenoldopam证实了对血管加压的剂量反应曲线的平行位移对去甲肾上腺素的反应。 pA2 values were determined by Schild analysis for dopexamine, fenoldopam and prazosin antagonism of noradrenaline in the presence of neuronal (cocaine, 10(-5) M) and extraneuronal uptake blockade (metanephrine, 10(-5) M). The values were 6.23, 6.02 and 8.91, respectively. Schild plot slopes of unity were obtained for dopexamine and fenoldopam indicating competitive antagonism. A slope of greater than unity for prazosin may be explained by the lack of equilibrium conditions associated with bolus doses of noradrenaline, the responses of which are affected more by the high affinity antagonist, prazosin, than the two lower affinity antagonists. 6. This study has demonstrated that renal vasodilator responses to the D,-receptor agonists, dopexamine and fenoldopam, are due to a brief antagonism of the alpha-adrenoceptor-mediated vasoconstriction induced by noradrenaline. This presumably masks any direct D1-receptor-mediated vasodilatation.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Fenoldopam	Alpha-1A肾上腺素能受体	蛋白质	人类	未知的	抑制剂	细节
Fenoldopam	Alpha-1B肾上腺素能受体	蛋白质	人类	未知的	抑制剂	细节
Fenoldopam	Alpha-1D肾上腺素能受体	蛋白质	人类	未知的	抑制剂	细节
Fenoldopam	Alpha-2A肾上腺素能受体	蛋白质	人类	未知的	拮抗剂	细节
Fenoldopam	Alpha-2B肾上腺素能受体	蛋白质	人类	未知的	拮抗剂	细节
Fenoldopam	Alpha-2C肾上腺素能受体	蛋白质	人类	未知的	拮抗剂	细节