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兔血管中5-羟色胺的受体:兔胸主动脉中α肾上腺素能受体的激活

Receptors for 5-hydroxytryptamine in rabbit blood vessels: activation of alpha adrenoceptors in rabbit thoracic aorta.

作者信息

Purdy R E, Murray D L, Stupecky G L

出版信息

J Pharmacol Exp Ther. 1987 Feb;240(2):535-41.

PMID:2879909
Abstract

Experiments were carried out to identify the receptors mediating the contraction of the rabbit thoracic aorta to 5-hydroxytryptamine (5-HT). Isolated aortic rings were mounted in tissue baths for the measurement of isometric contraction and 5-HT dose-response curves were obtained in the presence and absence of receptor antagonists. Prazosin, 1 X 10(-7) M, or 30-min pretreatment with 1 X 10(-5) M benextramine had no effect on the contractile response of aorta to 5-HT up to 1 X 10(-5) M, whereas 2 brom-D-lysergic acid diethylamide, 1 X 10(-7) M, shifted the 5-HT dose-response curve far to the right. Alpha receptor blockade with either prazosin or benextramine in the presence of 2 brom-D-lysergic acid diethylamide produced a greater blockade than that caused by 2 brom-D-lysergic acid diethylamide alone. When 5-HT dose-response curves were extended to 1 X 10(-3) M, three phases were identified. The first, a dose-related contraction, was mediated exclusively by serotonergic receptors. The second, a relaxation to approximately 40% of maximum, occurred at 1 X 10(-5) M and appeared to result from the rapid development of tachyphylaxis. The third phase was a dose-related contraction to concentrations of 5-HT above 1 X 10(-5) M and was inhibited by either prazosin or pretreatment with benextramine. Similar results were obtained in aortic rings from reserpine-pretreated rabbits. It is concluded that the contractile response to concentrations of 5-HT below 1 X 10(-5) M is mediated exclusively by serotonergic receptors.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

进行了实验以确定介导兔胸主动脉对5-羟色胺(5-HT)收缩反应的受体。将离体主动脉环安装在组织浴中以测量等长收缩,并在存在和不存在受体拮抗剂的情况下获得5-HT剂量反应曲线。1×10^(-7)M的哌唑嗪或用1×10^(-5)M苄胺预处理30分钟,对高达1×10^(-5)M的主动脉对5-HT的收缩反应没有影响,而1×10^(-7)M的2-溴-D-麦角酸二乙酰胺使5-HT剂量反应曲线大幅右移。在存在2-溴-D-麦角酸二乙酰胺的情况下,用哌唑嗪或苄胺进行α受体阻断产生的阻断作用比单独使用2-溴-D-麦角酸二乙酰胺引起的阻断作用更大。当5-HT剂量反应曲线扩展到1×10^(-3)M时,确定了三个阶段。第一个阶段是与剂量相关的收缩,完全由血清素能受体介导。第二个阶段是在1×10^(-5)M时松弛至最大收缩的约40%,似乎是由快速产生的耐受性引起的。第三个阶段是对高于1×10^(-5)M的5-HT浓度的与剂量相关的收缩,可被哌唑嗪或苄胺预处理抑制。在利血平预处理的兔的主动脉环中也获得了类似结果。得出结论,对低于1×10^(-5)M的5-HT浓度的收缩反应完全由血清素能受体介导。(摘要截短至250字)

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