Alpha 1 (alpha 1)-adrenoceptors can be found at numerous end organs in the autonomic nervous system, especially vascular smooth muscle. The tonic sympathetic activation of vascular alpha 1-adrenoceptors maintains vascular resistance and is vital to the regulation of arterial pressure. Recent evidence clearly demonstrates that alpha 1-adrenoceptors are a heterogenous class of receptors and that each subtype may subserve specific cardiovascular functions. Elucidation of the physiological role of each subtype in the regulation of vascular resistance and arterial pressure will enhance our understanding of the cardiovascular system and may facilitate the development of therapeutics with improved efficacy and tolerability.