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Abstract
Central imidazoline (I1)-receptors have been recognised as targets of a new class of centrally acting antihypertensives. The stimulation of these I1-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 α-methyl-DOPA, the side-effects profile of the I1-receptor stimulants is significantly better. The imidazoline (I1)-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 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.