5 Ht2C Receptor is an important component in the neurobiology of neurodegenerative diseases. This page provides detailed information about its structure, function, and role in disease processes.
Gq-coupled serotonin receptor regulating mood, appetite, and motor control
The HTR2C protein is encoded by the HTR2C gene and is a member of the Serotonin receptor family (Class A GPCR). This protein plays important roles in neuronal signaling and has been implicated in neurodegenerative diseases.
| Attribute | Value |
|---|---|
| Protein Name | 5-HT2C Receptor |
| Gene | HTR2C |
| UniProt ID | P28335 |
| PDB Structures | 6WH4, 7R0F |
| Molecular Weight | 58 kDa |
| Subcellular Localization | Plasma membrane, postsynaptic densities |
| Protein Family | Serotonin receptor family (Class A GPCR) |
The HTR2C protein contains seven transmembrane helices typical of class A GPCRs, with an extracellular N-terminus and intracellular C-terminus. The ligand-binding pocket is located within the transmembrane domain. Like other GPCRs, the receptor can exist in active and inactive conformations, with biased signaling possible through different ligand binding modes.
The 5-HT2C receptor is a Gq-coupled GPCR highly expressed in the choroid plexus, hypothalamus, basal ganglia, and cortex. Unlike 5-HT2A, 5-HT2C activation inhibits dopamine release in the mesolimbic and mesocortical pathways, making it an important regulator of reward and motivation. The receptor plays critical roles in mood regulation, anxiety, appetite control, and sleep-wake cycles. 5-HT2C receptors undergo constitutive activity and can be regulated by RNA editing (five editing sites), which alters their signaling efficacy. In the hypothalamus, 5-HT2C receptors regulate appetite and energy homeostasis through melanocortin signaling.
Depression (therapeutic target), Anxiety (altered signaling), Prader-Willi Syndrome (hyperphagia), Schizophrenia (antipsychotic target), Alzheimer's Disease (neuropsychiatric symptoms), Parkinson's Disease (levodopa-induced dyskinesias)
Agomelatine - 5-HT2C antagonist and melatonin receptor agonist approved for depression. Lorcaserin (withdrawn) was a 5-HT2C agonist for obesity. 5-HT2C antagonists enhance dopamine release and may reduce levodopa-induced dyskinesias in PD. Tramadol and mCPP act as 5-HT2C agonists. Novel 5-HT2C modulators in development for metabolic and neuropsychiatric disorders.
The study of 5 Ht2C Receptor has evolved significantly over the past decades. Research in this area has revealed important insights into the underlying mechanisms of neurodegeneration and continues to drive therapeutic development.
Historical context and key discoveries in this field have shaped our current understanding and will continue to guide future research directions.
5-HT2C receptors are expressed in:
5-HT2C couples to Gq proteins:
Alzheimer's Disease:
Parkinson's Disease:
Huntington's Disease:
Agonists:
Antagonists: