5-HT7 receptors: current knowledge and future prospects

Identification of three splice Variants of the 5-HT7 receptor suggests a po ssible diversity in 5-HT7 receptor action. Indeed, 5-HT7 receptors have bee n implicated in the pathophysiology of several disorders; they play a role in smooth muscle relaxation within the vasculature and in the gastrointesti nal tract However, most of these assignments are derived from receptor loca lization studies and investigations using nonselective ligands, and are the refore mainly suggestive. The development of selective 5-HT7 receptor antag onists will he of utmost importance in determining the actual physiological and pharmacological roles of this receptor. Major challenges of 5-HT7 rece ptor research are determination of the transcriptional regulation of the ge ne encoding the 5-HT7 receptor and elucidation of the differences in regula tion and signalling of its four gene products.