Antihypertensive drugs interacting with central imidazoline (I1)-receptors.

Research paper by P A PA van Zwieten

Indexed on: 05 Jul '05Published on: 05 Jul '05Published in: Expert opinion on investigational drugs


Central imidazoline (I(1))-receptors have been recognised as targets of a new class of centrally acting antihypertensives. The stimulation of these I(1)-receptors induces peripheral sympatho-inhibition and a reduction of (elevated) blood pressure. Moxonidine and rilmenidine are the prototypes of this new class of centrally acting antihypertensives. These imidazoline receptor stimulants are effective antihypertensives with a haemodynamic profile which is attractive from a pathophysiological point of view. Since both moxonidine and rilmenidine have a much weaker affinity for central (2)-adrenoceptors than classic centrally acting drugs, for example, clonidine and alpha-methyl-DOPA, the side-effects profile of the I(1)-receptor stimulants is significantly better. The imidazoline (I(1))-receptor stimulants are the subject of the current survey. They appear to offer the possibility of developing centrally acting antihypertensives with the same attractive haemodynamic characteristics as the classic alpha(2)-adrenoceptor stimulants, but with clearly better tolerability. Their potential use in the treatment of congestive heart failure and the metabolic syndrome is subject to clinical investigation.