Evidence has accumulated to suggest the 5-HT₇ receptor is involved in the regulation of limbic processes, circadian rhythms and sensory processing. Interest in the 5-HT₇ receptor field has recently increased as new findings suggest its implication in the pathogenesis of migraine and modulation of sensory afferents and sympathetic efferents. Although the possible involvement of the 5-HT₇ receptor in human pathology and therapeutics was initially inferred from therapies displaying high affinity at the 5-HT₇ receptor e.g. antipsychotic drugs, the recent availability of selective 5-HT₇ receptor antagonists will undoubtedly shed light into the physiological and pathophysiological significance of this receptor. The aim of this review is to discuss the current status of 5-HT₇  receptor in terms of its possible role in physiological and pathophysiological processes. As one of the targets of several currently useful medications, selective blockade/stimulation of the 5-HT₇ receptor is addressed as a novel potential therapeutic approach. A brief overview of novel selective 5-HT₇ receptor antagonists is also provided.