非诺多泮（SKF 82526）对血管5-羟色胺2受体激动活性的分析。
Analysis of the agonist activity of fenoldopam (SKF 82526) at the vascular 5-HT2 receptor.
作者信息
Christie M I, Harper D, Smith G W
机构信息
Fisons plc, Department of Pharmacology, Loughborough, Leicestershire.
出版信息
Br J Pharmacol. 1992 Dec;107(4):1008-12. doi: 10.1111/j.1476-5381.1992.tb13399.x.
Abstract
- The 5-HT2 receptor agonist activity of fenoldopam (SKF 82526) was characterized in the rabbit isolated aorta preparation. 2. Fenoldopam was an agonist at the vascular 5-HT2 receptor with lower affinity and efficacy than the naturally occurring agonist 5-hydroxytryptamine (5-HT). Fenoldopam had an affinity (pKA) of 5.84 +/- 0.04 and efficacy (tau) of 0.57 +/- 0.04, whereas 5-HT had a pKA of 6.65 +/- 0.12 and tau of 2.66 +/- 0.41. 3. The constrictor effects of fenoldopam and 5-HT were competitively antagonized by the 5-HT2 antagonist, ketanserin, with pKB values of 8.81 +/- 0.11 and 8.83 +/- 0.10 respectively. 4. Prior incubation with fenoldopam produced a concentration-related rightward shift of a subsequent 5-HT concentration-response curve. This inhibition was specific for 5-HT since constrictor responses to angiotensin II were unaffected. 5. This study indicates that the D1 receptor agonist, fenoldopam, acts as an agonist at the vascular 5-HT2 receptor, but with an affinity and efficacy less than that of the naturally occurring agonist, 5-HT.
摘要
- 在兔离体主动脉制备中对非诺多泮（SKF 82526）的5-羟色胺2（5-HT2）受体激动剂活性进行了表征。2. 非诺多泮是血管5-HT2受体的激动剂，其亲和力和效能低于天然激动剂5-羟色胺（5-HT）。非诺多泮的亲和力（pKA）为5.84±0.04，效能（τ）为0.57±0.04，而5-HT的pKA为6.65±0.12，τ为2.66±0.41。3. 5-HT2拮抗剂酮色林竞争性拮抗非诺多泮和5-HT的收缩效应，pKB值分别为8.81±0.11和8.83±0.10。4. 预先用非诺多泮孵育会使随后的5-HT浓度-反应曲线产生浓度相关的右移。这种抑制对5-HT具有特异性，因为对血管紧张素II的收缩反应未受影响。5. 本研究表明，D1受体激动剂非诺多泮在血管5-HT2受体上起激动剂作用，但其亲和力和效能低于天然激动剂5-HT。
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2
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3
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4
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5
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