Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.

ABSTRACT: Pharmacological studies have suggested that I1-imidazoline receptors are involved in the regulation of cardiovascular function and that selective I1-agonists, devoid of the side effects associated with the common hypotensive α2-adrenoreceptor agonists, might be considered as a second generation of centrally acting antihypertensives. Therefore, in the present study, inspired by the antihypertensive behavior of our selective I1-agonist 4, we designed, prepared, and studied the novel analogues 5-9. A selective I1-profile, associated with significant hemodinamic effects, was displayed by 5, 8, and 9. Interestingly, the highest potency and longest lasting activity displayed by 8 (carbomethyline) suggested that van der Waals interactions, promoted by the ortho methyl decoration of its aromatic m

SUBMITTER: Del Bello F 

PROVIDER: S-EPMC4434467 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature