The imidazoline receptors have recently been discovered to be involved in central nervous system control of blood pressure (I-1 receptor) and in neuroprotection for cerebral ischemia (I-2 receptor). A new class of central-acting antihypertensive agents has been developed, the imidazoline receptor agonists (rilmenidine and moxonidine), which control blood pressure effectively without the adverse effects of sedation and mental depression that are usually associated with central-acting antihypertensives. This new generation of central-acting antihypertensive agents are highly selective for the imidazoline receptor, while having a low affinity for alpha 2-adrenergic receptors.