5-hydroxytryptamine receptor 7 (5-HT7R) (5-HT7R)

The 5-hydroxytryptamine receptor 7 (5-HT7 receptor) is a G protein-coupled receptor (GPCR) that primarily signals through the stimulatory Gs protein to increase intracellular cyclic AMP (cAMP) levels [2, 6]. It is widely expressed in the central nervous system, particularly in the thalamus, hypothalamus, and hippocampus, as well as in peripheral tissues like the gastrointestinal tract and blood vessels [2, 12, 15]. Biologically, the 5-HT7 receptor plays a critical role in regulating circadian rhythms, thermoregulation, learning, memory, and smooth muscle relaxation [1, 2, 11]. Dysregulation of this receptor is implicated in various conditions, including major depressive disorder, anxiety, schizophrenia, and irritable bowel syndrome [3, 4, 13]. In oncology, the receptor has emerged as a potential biomarker and therapeutic target in triple-negative breast cancer, where its activation promotes cell proliferation via the FOXM1 pathway [16]. Pharmacologically, 5-HT7 receptor antagonists like lurasidone and vortioxetine are used in the treatment of psychiatric disorders, while selective agonists are being explored for their potential to enhance cognitive function and manage sleep disturbances [1, 13, 15].

Other names

5-HT7HTR7Serotonin receptor 75-HT-X

Agonism, Antagonism, Inverse agonism