Docherty J R, Hyland L
Br J Pharmacol. 1986 Sep;89(1):77-81. doi: 10.1111/j.1476-5381.1986.tb11122.x.
We have examined the effects of antagonists on the isometric contraction of the human saphenous vein produced by 5-hydroxytryptamine (5-HT). The 5-HT2-antagonist ketanserin (1 microM) had little effect on the lower part of the concentration-response curve to 5-HT, but markedly shifted the upper part of the curve. Yohimbine caused an approximately parallel shift of the concentration-response curve to 5-HT, with a pA2 of 5.48, much lower than its pA2 against noradrenaline in the absence (6.36) or presence (7.06) of cocaine. It is concluded that there are two components to the contractile response to 5-HT in human saphenous vein: at low concentrations 5-HT activates a yohimbine-sensitive receptor, and at higher concentrations 5-HT activates a 5-HT2-receptor.
我们研究了拮抗剂对5-羟色胺(5-HT)引起的人隐静脉等长收缩的影响。5-HT2拮抗剂酮色林(1微摩尔)对5-HT浓度-反应曲线的下部影响很小,但使曲线的上部明显上移。育亨宾使5-HT浓度-反应曲线近似平行上移,其pA2为5.48,远低于其在不存在(6.36)或存在(7.06)可卡因时对去甲肾上腺素的pA2。结论是人隐静脉对5-HT的收缩反应有两个成分:低浓度时5-HT激活对育亨宾敏感的受体,高浓度时5-HT激活5-HT2受体。