Characterization of imidazoline receptors in blood vessels for the development of antihypertensive agents

Mei Fen Chen, Jo Ting Tsai, Li Jen Chen, Tung Pi Wu, Jia Jang Yang, Li Te Yin, Yu Lin Yang, Tai An Chiang, Han Lin Lu, Ming Chang Wu

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Abstract

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

Original languageEnglish
Article number182846
JournalBioMed Research International
Volume2014
DOIs
Publication statusPublished - 2014

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ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Immunology and Microbiology(all)
  • Medicine(all)

Cite this

Chen, M. F., Tsai, J. T., Chen, L. J., Wu, T. P., Yang, J. J., Yin, L. T., Yang, Y. L., Chiang, T. A., Lu, H. L., & Wu, M. C. (2014). Characterization of imidazoline receptors in blood vessels for the development of antihypertensive agents. BioMed Research International, 2014, [182846]. https://doi.org/10.1155/2014/182846