Fujiwara T, Chiba S
Department of Pharmacology, Shinshu University School of Medicine, Matsumoto, Japan.
Jpn J Pharmacol. 1993 Mar;61(3):171-6. doi: 10.1254/jjp.61.171.
The stainless steel cannula inserting method was used to observe vascular effects of alpha-adrenoceptor agonists, phenylephrine (PE), methoxamine (ME), clonidine (CL) and xylazine (XY), on the isolated, perfused rabbit common carotid, renal and femoral arteries. PE and ME induced a dose-dependent vasoconstriction that was readily suppressed by treatment with bunazosin, an alpha 1-adrenoceptor blocker. CL induced a constriction only in common carotid arteries, and this was readily suppressed by bunazosin. In preparations preconstricted by phenylephrine, CL and XY dose-dependently induced vasodilations in the 3 types of arteries, and these vasodilations were not modified by a potent alpha 2-adrenoceptor antagonist, midaglizole. In preparations preconstricted by prostaglandin F2 alpha, CL and and XY did not produce any significant vasodilation, but CL induced a vasoconstriction in common carotid arteries that was completely blocked by bunazosin. Thus, it is concluded that: 1) alpha 1-adrenoceptors are functionally predominant in rabbit peripheral arteries, 2) the alpha 2-adrenoceptor agonist-induced vasodilation may be due to an antagonistic action towards alpha 1-mediated constrictions, and 3) clonidine has alpha 1-adrenoceptor stimulating properties in rabbit common carotid artery but not in renal and femoral arteries.
采用不锈钢套管插入法,观察α-肾上腺素能受体激动剂去氧肾上腺素(PE)、甲氧明(ME)、可乐定(CL)和赛拉嗪(XY)对离体灌注兔颈总动脉、肾动脉和股动脉的血管作用。PE和ME引起剂量依赖性血管收缩,用α1-肾上腺素能受体阻滞剂布那唑嗪治疗可轻易抑制这种收缩。CL仅在颈总动脉中引起收缩,且布那唑嗪可轻易抑制这种收缩。在由去氧肾上腺素预收缩的制剂中,CL和XY在3种类型的动脉中剂量依赖性地引起血管舒张,且这些血管舒张不受强效α2-肾上腺素能受体拮抗剂咪达格列唑的影响。在由前列腺素F2α预收缩的制剂中,CL和XY未产生任何明显的血管舒张,但CL在颈总动脉中引起血管收缩,且布那唑嗪可完全阻断这种收缩。因此,得出以下结论:1)α1-肾上腺素能受体在兔外周动脉中功能上占主导地位;2)α2-肾上腺素能受体激动剂诱导的血管舒张可能是由于对α1介导的收缩的拮抗作用;3)可乐定在兔颈总动脉中具有α1-肾上腺素能受体刺激特性,但在肾动脉和股动脉中不具有。