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.
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