Rilmenidine

Description

Rilmenidine is a new antihypertensive agent with a selective alphaz-agonist/antagonist profile, reportedly useful in the management of mild to moderate hypertension. Its fmt-line indication is possible because of the clear dissociation of its antihypertensive activity from other neurophannacological effects.

Chemical Properties

water soluble

Originator

Servier (France)

Uses

I1-imidazoline binding site ligand and a2-adrenoceptor agonist, exhibits higher I1 vs. a2 selectivity than clonidine

Definition

ChEBI: Rilmenidine is an isourea.

brand name

Hyperium

Biological Activity

I 1 -imidazoline binding site selective ligand and α 2 -adrenoceptor agonist. Possesses greater I 1 vs α 2 selectivity than the prototypical compound, clonidine.

Metabolic pathway

In short-term rat hepatocyte cultures, oxaminozoline is metabolized and its four metabolites resulting from oxidation or hydrolysis are identified, three of which are identical to those reported in vivo. The presence of an additional minor metabolite in culture may be due to the higher metabolic rate of oxaminozoline in this model system.