Imidazoline Receptor Agonists: Moxonidine and Rilmenidine

Abstract: Centrally acting sympatholytics have been used to treat hypertension. Two subtypes of the imidazoline receptor have been identified. These receptors are present in various locations in the body. Moxonidine and rilmenidine are the newer generation of imidazoline receptor agonists. Moxonidine is a selective I1 receptor agonist. It is approved for use in hypertension and is under investigation in cardiac failure. Other uses are being investigated. Rilmenidine is being used in hypertension and is comparable to reference antihypertensives. These drugs lower blood pressure without the adverse effects of the older generation of sympatholytics like clonidine. Very highly selective drugs for the imidazoline receptors are under development.

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