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体外比较5-羟色胺诱导的人基底动脉条与大鼠主动脉条收缩的分析。

Analysis of the 5-hydroxytryptamine induced contraction of the human basilar arterial strip compared with the rat aortic strip in vitro.

作者信息

Forster C, Whalley E T

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):12-7. doi: 10.1007/BF00491471.

Abstract
  1. Experiments were performed to investigate the nature of the contraction produced by 5-hydroxytryptamine in the human basilar arterial strip in vitro and to compare it with that produced in the rat aortic strip in vitro. 2) The human basilar arterial strip was found to be significantly more sensitive to 5-HT compared to the rat aortic strip. 3) Methysergide, cyproheptadine and methergoline were competitive, selective antagonists against 5-HT on the rat aorta with pA2 values of 7.97, 8.76 and 9.49 respectively. In contrast 5-HT was antagonised by these agents in a manner which was not competitive on the human basilar artery. Both 5-HT and NA were antagonised by BW 501 C67 (alpha-anilino-N-2-m-chlorphenoxy propylacetamide hydrochloride) in a manner which was not competitive on both rat aortic and human basilar arterial strips. 4) Phentolamine (10(-7) to 10(-5) M) was found to be a competitive antagonist against noradrenaline on both the rat aortic strip (pA2 6.9) and the human basilar arterial strip (pA2 7.3). Phentolamine at 10(-5) M shifted the 5-HT curve on the human basilar artery to the right with a reduction in maximum response. 5) Methysergide (10(-9) to 10(-4) M) was found to possess contractile activity on some human basilar arterial strips, the maximum response being approximately 60% of that produced by 5-HT. Phentolamine at 10(-5) M shifted the dose-response curve to methysergide to the right with a slight reduction in the maximum response obtained. 6) The results from this study suggest that the receptor(s) mediating 5-HT-induced contraction of the human basilar artery may be different from the classical "D-receptor" which mediates contraction to 5-HT on the rat aorta.
摘要
  1. 进行实验以研究5-羟色胺在体外对人基底动脉条产生的收缩性质,并将其与在体外大鼠主动脉条产生的收缩进行比较。2) 发现人基底动脉条对5-羟色胺的敏感性明显高于大鼠主动脉条。3) 甲基麦角新碱、赛庚啶和麦角乙脲是大鼠主动脉上对5-羟色胺的竞争性、选择性拮抗剂,其pA2值分别为7.97、8.76和9.49。相比之下,这些药物在人基底动脉上对5-羟色胺的拮抗方式不具有竞争性。5-羟色胺和去甲肾上腺素在大鼠主动脉条和人基底动脉条上均被BW 501 C67(α-苯胺基-N-2-间氯苯氧基丙基乙酰胺盐酸盐)以非竞争性方式拮抗。4) 发现酚妥拉明(10⁻⁷至10⁻⁵M)在大鼠主动脉条(pA2 6.9)和人基底动脉条(pA2 7.3)上均是去甲肾上腺素的竞争性拮抗剂。10⁻⁵M的酚妥拉明使5-羟色胺在人基底动脉上的曲线右移,最大反应降低。5) 发现甲基麦角新碱(10⁻⁹至10⁻⁴M)在一些人基底动脉条上具有收缩活性,最大反应约为5-羟色胺产生反应的60%。10⁻⁵M的酚妥拉明使甲基麦角新碱的剂量-反应曲线右移,获得的最大反应略有降低。6) 本研究结果表明,介导5-羟色胺诱导人基底动脉收缩的受体可能不同于介导大鼠主动脉对5-羟色胺收缩反应的经典“D受体”。

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