Purdy R E, Hurlbut D E, Rains L A
Blood Vessels. 1981;18(1-2):16-27. doi: 10.1159/000158334.
The effects of N,N'-bis-(O-methoxybenzylaminohexyl)-cystamine tetrahydrochloride (BHC), 2-brom-d-lysergic acid diethylamide (BOL) and prazosin on 5-hydroxytryptamine (5-HT) dose-response curves in rabbit ear artery and thoracic aorta were determined. BHC, an irreversible alpha-adrenoceptor antagonist, and prazosin had no substantial effect while BOL shifted the 5-HT dose-response curve to the right in aorta. BHC shifted the curve to the right and reduced maximal response to 5-HT in ear artery. BOL shifted the curve to the right only above 10(-6) M 5-HT in control, but at all concentrations studied in BHC-pretreated ear arteries. In vitro denervation of the ear artery with 6-hydroxydopamine did not significantly alter the 5-HT dose-response curve, nor the effect of BHC on that curve. On the other hand, desipramine decreased the contractile response to high concentrations of 5-HT in non-denervated ear arteries. Prazosin increased the 5-HT threshold and slope of the curve in the ED50 region, but had no inhibitory effect on contractile responses above 3 x 10(-7) M 5-HT or on maximal response. It is concluded that 5-HT acts exclusively on 5-HT receptors in aorta, but on both alpha-adrenergic and 5-HT receptors in ear artery. 5-HT also possesses a small indirect sympathomimetic action at high concentrations in the ear artery. Prazosin has no effect on 5-HT receptors in either vessel and blocks the alpha-adrenoceptor stimulation by 5-HT in ear artery.
测定了N,N'-双(O-甲氧基苄基氨基己基)-胱胺四盐酸盐(BHC)、2-溴-d-麦角酸二乙酰胺(BOL)和哌唑嗪对兔耳动脉和胸主动脉中5-羟色胺(5-HT)剂量反应曲线的影响。BHC是一种不可逆的α-肾上腺素能受体拮抗剂,与哌唑嗪均无显著作用,而BOL可使主动脉中5-HT剂量反应曲线右移。BHC使兔耳动脉中5-HT剂量反应曲线右移,并降低对5-HT的最大反应。在对照中,BOL仅在5-HT浓度高于10^(-6) M时使曲线右移,但在经BHC预处理的耳动脉中,在所有研究浓度下均使曲线右移。用6-羟基多巴胺对耳动脉进行体外去神经处理,并未显著改变5-HT剂量反应曲线,也未改变BHC对该曲线的作用。另一方面,地昔帕明可降低未去神经耳动脉对高浓度5-HT的收缩反应。哌唑嗪提高了ED50区域内5-HT曲线的阈值和斜率,但对浓度高于3×10^(-7) M的5-HT收缩反应或最大反应无抑制作用。结论为,5-HT仅作用于主动脉中的5-HT受体,但在耳动脉中作用于α-肾上腺素能受体和5-HT受体。在耳动脉中,高浓度的5-HT还具有轻微的间接拟交感神经作用。哌唑嗪对两种血管中的5-HT受体均无作用,并可阻断耳动脉中5-HT对α-肾上腺素能受体的刺激。