Since the subtypes of α(1)-adrenergic receptor have been thoroughly determined, to date medicinal chemists raise their deliberation on how to conceive selective α(1)-adrenergic receptor antagonist with the minimal side effects. It needs to be well recognized that natural products can exist as a significant source of drug leads, thus portraying a consequential capacity in drug design and development. The current review article would like to present a comprehensive survey on natural products, mainly including alkaloids and flavonoids, which exhibit α(1)-adrenergic receptor antagonistic activities.