Alpha blockers have been prescribed for the treatment of benign prostatic hyperplasia (BPH) since 1976. Recently, several multicenter, randomized, placebo-controlled studies have unequivocally established the safety and efficacy of long-acting selective alpha) blockers for the treatment of BPH. The advantages of the long-acting selective alpha1C blockers over the non-selective alpha blockers include better tolerance and compliance. The efficacy of alpha blockade is presumably achieved by receptor-mediated relaxation of prostatic smooth muscle. The tension of prostatic smooth muscle has recently been shown to be mediated by the alpha1c subtype. The development of alphas selective antagonists may further improve the efficacy, tolerance, and compliance of this pharmacologic strategy for treating BPH.