The nicotinic acetylcholine receptors present in the mammalian brain have received less attention than those in other areas of the nervous system. However, recent studies have reported the pharmacological character and regional distribution of a high-affinity binding of [³H]acetylcholine or[³H]nicotine. In this review, the pharmacological characters and physiological functions of the brain nicotinic receptors were discussed with special reference to central cardiovascular regulation.