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离体犬肠系膜动脉和静脉突触后α-肾上腺素能受体的药理学特性

Pharmacological characterization of the postsynaptic alpha-adrenoceptors in isolated canine mesenteric arteries and veins.

作者信息

Itoh H, Kohli J D, Rajfer S I

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1987 Jan;335(1):44-9. doi: 10.1007/BF00165034.

Abstract

This investigation was undertaken to characterize the postsynaptic alpha-adrenoceptors in isolated canine mesenteric arterial and venous preparations. Contractile responses to cumulative additions of phenylephrine (selective alpha 1-adrenoceptor agonist), UK-14,304 (selective alpha 2-adrenoceptor agonist), noradrenaline (non-selective alpha-adrenoceptor agonist), and dopamine (non-selective alpha-adrenoceptor agonist) were measured in the presence and absence of rauwolscine, a selective alpha 2-antagonist, and terazosin, a selective alpha 1-antagonist. Phenylephrine was a more potent agonist in the mesenteric artery than in the mesenteric vein; UK-14,304 exhibited the opposite profile of activity. Terazosin was a more potent antagonist than rauwolscine against each of the agonists, except dopamine, in the mesenteric artery but rauwolscine was more potent than terazosin in the vein. Terazosin and rauwolscine were equipotent in inhibiting the contractile responses to dopamine in the artery while rauwolscine was more potent than terazosin in the vein. The pA2 values measured in both vessels failed, however, to demonstrate a high selectivity for either alpha-adrenoceptor antagonist. These results suggest that the alpha-adrenoceptors in the canine mesenteric artery and vein exhibit pharmacological characteristic typical of both alpha 1- and alpha 2-adrenoceptor subtypes.

摘要

本研究旨在表征分离的犬肠系膜动脉和静脉制剂中的突触后α-肾上腺素能受体。在存在和不存在选择性α2拮抗剂萝芙辛和选择性α1拮抗剂特拉唑嗪的情况下,测量对去氧肾上腺素(选择性α1-肾上腺素能受体激动剂)、UK-14,304(选择性α2-肾上腺素能受体激动剂)、去甲肾上腺素(非选择性α-肾上腺素能受体激动剂)和多巴胺(非选择性α-肾上腺素能受体激动剂)累积添加的收缩反应。去氧肾上腺素在肠系膜动脉中比在肠系膜静脉中是更强效的激动剂;UK-14,304表现出相反的活性特征。除多巴胺外,特拉唑嗪在肠系膜动脉中对每种激动剂都是比对萝芙辛更强效的拮抗剂,但在静脉中萝芙辛比特拉唑嗪更有效。特拉唑嗪和萝芙辛在抑制动脉中对多巴胺的收缩反应方面效力相当,而在静脉中萝芙辛比特拉唑嗪更有效。然而,在两个血管中测得的pA2值未能证明对任何一种α-肾上腺素能拮抗剂具有高选择性。这些结果表明,犬肠系膜动脉和静脉中的α-肾上腺素能受体表现出α1-和α2-肾上腺素能受体亚型典型的药理学特征。

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