Circulatory effect of TCS-80, a new imidazoline compound, in rats

摘要

Background: Synthesis and hypotensive properties of centrally acting imidazoline agents: 1-[(imidazolidin-2-yl)imino]-1H-indazole (Marsanidine) and 7-chloro-1-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-1H-indazole (TCS-80) were tested in rats. We have recently synthesized two novel Marsanidine analogues which decrease blood pressure and heart rate in rats: 1-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-1H-indole (TCS-54), and 7-chloro-1-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-1H-indole (TCS-213). Among all these analogues, compound TCS-80 exhibits the highest affinity to I-1-imidazoline receptors and the lowest alpha(2)/I-1 selectivity ratio. The observed cardiovascular effects of the compounds might be mediated through alpha(2)-adrenergic and I-1-imidazoline receptors and subsequent decrease of the symphathetic nerve activity. The present studies were performed to determine whether alpha(2)-adrenergic and/or I-1-imidazoline receptors are involved in the decrease of blood pressure and heart rate induced by Marsanidine, TCS-54, TCS-80, and TCS-213 in rats.