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5-hydroxytryptamine receptor 7 (5-HT7 receptor)

Target: 5-HT7 receptor
Molecular classification: G protein-coupled receptor, GPCR

Overview

The 5-hydroxytryptamine receptor 7 (5-HT7 receptor) is a G protein-coupled receptor binding serotonin. It is one of the most recently identified serotonin receptors and is coupled primarily to Gs protein, stimulating adenylyl cyclase, and also to G12-protein, activating Rho family GTPases. It plays roles in neurotransmission, circadian rhythms, neuronal development, and has been implicated in mood disorders, cognitive disorders, cancer, and other conditions. Many drugs interact with it, including selective antagonists, antipsychotics, and antidepressants. Blockade of 5-HT7 receptors is being investigated as a therapeutic approach for conditions like depression and cognitive deficits.

Other names: 5-hydroxytryptamine receptor 7

Mechanism of action

The 5-HT7 receptor is primarily coupled to Gs protein, stimulating adenylyl cyclase and increasing cAMP. It also couples to G12-protein, activating Rho family GTPases for cytoskeletal reorganization and neurite outgrowth. Therapeutic approaches primarily focus on blockade of the receptor.

Biological functions

Functions in serotonergic signaling pathways in the brain (Neurotransmission)Controls body temperature and regulates sleep and circadian rhythms (Regulation of circadian rhythms)Promotes formation of dendritic spines and accelerates synaptogenesis in hippocampal neurons (Neuronal development)Induces pronounced filopodia formation via a Cdc42-mediated pathway and RhoA-induced cell rounding in neuroblastoma cells (Morphogenic action)Stimulates neurite growth in striatal and cortical neuronal cultures through ERK and Cdk5 pathways (Neurite outgrowth)

Disease associations

Implicated in depression (Mood disorders)Blockade may be beneficial against schizophrenia-like cognitive deficits (Cognitive disorders)Identified as a biomarker and poor prognostic factor in triple-negative breast cancer, where it induces proliferation through FOXM1 (Cancer)Potential involvement in nociception, epilepsy, migraine, autism spectrum disorders, and Rett Syndrome (Other conditions)

Interacting drugs

SB-269970

28 more in the full profile.

Biomarkers

Biomarker and poor prognostic factor in triple-negative breast cancer

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