5-hydroxytryptamine receptor 7 (5-HT7) (5-HT7)

The 5-hydroxytryptamine receptor 7 (5-HT7) is a member of the G protein-coupled receptor (GPCR) superfamily and is the most recently identified serotonin receptor subtype [1]. It is primarily coupled to the Gs protein, which stimulates adenylate cyclase activity, leading to an increase in intracellular cyclic AMP (cAMP) levels [2]. This receptor is widely expressed in the central nervous system, particularly in the hypothalamus, thalamus, and hippocampus, where it plays a vital role in regulating circadian rhythms, thermoregulation, and cognitive functions such as learning and memory [1][3]. In the periphery, 5-HT7 receptors are found in the gastrointestinal tract and blood vessels, contributing to smooth muscle relaxation [4]. Given its involvement in mood and sleep regulation, the 5-HT7 receptor has emerged as a key therapeutic target for treating major depressive disorder, anxiety, and schizophrenia [5]. Many clinically used atypical antipsychotics and antidepressants, such as lurasidone and vortioxetine, act as potent 5-HT7 antagonists, which is thought to contribute to their pro-cognitive and antidepressant effects [2][6].

Other names

HTR7Serotonin receptor 75-HT7 receptor5-hydroxytryptamine receptor 7 (adenylate cyclase-coupled)

Antagonism of the 5-HT7 receptor is the primary therapeutic mechanism for psychiatric applications, while agonism is explored for certain cognitive and gastrointestinal research [1][2][5].