The effect of 7-fluoro-marsanidine, a novel α2-adrenoceptor agonist, on extracellular noradrenaline in rat frontal cortex: A microdialysis study

1‐[(Imidazolidin‐2‐yl)imino]‐1H‐indoles as new hypotensive agents: synthesis and in vitro and in vivo biological studies

“…In comparison with the indazole ring system, the indole moiety is more lipophilic (log P indole 2.14 versus log P indazole 1.77) . Therefore, it appears that the more lipophilic nature and the higher α 2 ‐binding affinity of 7‐F‐indole 3g with respect to that of 7‐F‐indazole D may facilitate its ability to penetrate the brain–blood barrier and account for its more efficacious activity than 7‐F‐indazole D , which is a partial α 2 ‐AR agonist . In addition, under identical experimental conditions, changes of ΔMAP induced by 3g were much greater as compared to those of 3a and 3f (Table ; Figure S1) even though they showed higher activity at α 2 ‐ARs (Table ).…”

“…Indeed, imidazoline‐containing indazoles B exhibited hypotensive properties due to α 1 ‐AR antagonist activity, while their indole analogues C were described as partial α 2A ‐AR agonists showing clonidine‐like cardiovascular pattern . Furthermore, we described 1‐[(imidazolidin‐2‐yl)imino]‐1 H ‐indazoles D (Figure ; marsanidine‐like ligands), which proved to be hypotensive α 2 ‐AR agonists . However, pharmacological effects of the displacement of the indazole ring in compounds D with the indole ring system have not been investigated previously.…”