Characterization of Imidazoline Receptors in Blood Vessels for the Development of Antihypertensive Agents

摘要: It has been indicated that activation of peripheral imidazoline I2-receptor (I-2R) may reduce the blood pressure in spontaneously hypertensive rats (SHRs). Also, guanidinium derivatives show ability to activate receptors. Thus, it is special interest characterize I-2R using vessels for development antihypertensive agent(s). Six including agmatine, amiloride, aminoguanidine, allantoin, canavanine, and metformin were applied this study. Western blot analysis was used detecting expression receptor tissues Wistar rats. The isometric tension aortic rings isolated from male also estimated. on rat aorta identified. However, detection relaxation not observed except agmatine amiloride which induced a marked precontracted with phenylephrine or KCl. Both relaxations by attenuated glibenclamide at concentration enough block ATP-sensitive potassium (KATP) channels. Meanwhile, only agmatine-induced abolished BU224, selective antagonist I2-receptors. Taken together, we suggest can induce vascular through open KATP agmatine-like compound potential develop as new therapeutic agent hypertension future.