Target intelligence / Profile preview

Serotonin receptor (5-hydroxytryptamine receptor) (5-HT receptor)

Target
5-HT receptor
Molecular classification
G protein-coupled receptor, Ion channel, Receptor
01

Overview

Serotonin receptors, or 5-hydroxytryptamine (5-HT) receptors, are a diverse group of proteins that mediate the effects of the neurotransmitter serotonin across the central and peripheral nervous systems [3, 5]. They are primarily classified as G protein-coupled receptors (GPCRs), with the exception of the 5-HT3 receptor, which is a ligand-gated ion channel [3, 4]. These receptors are organized into seven distinct families (5-HT1 to 5-HT7) and play essential roles in regulating mood, sleep, appetite, cognition, and gastrointestinal motility [5, 8]. Dysregulation of serotonin receptor signaling is a hallmark of many psychiatric and neurological disorders, including major depressive disorder, anxiety, schizophrenia, and migraine [7, 12]. Consequently, they are among the most extensively studied therapeutic targets, with drugs ranging from triptans for migraines to atypical antipsychotics and antiemetics [5, 9]. The term “Serotonin receptor pathways” encompasses the various intracellular signaling cascades, such as the inhibition or stimulation of adenylyl cyclase and the activation of phospholipase C, that follow receptor activation [3, 6]. Therapeutic modulation of these pathways requires high subtype selectivity to avoid adverse effects like serotonin syndrome or cardiovascular complications [5, 10]. Overall, these receptors are central to both basic neurobiology and the pharmacological management of diverse human diseases [8, 12].

Other names
5-hydroxytryptamine receptor5-HT receptorSerotonin receptor familySerotonergic receptors
02

Mechanism of action

Agonism, Antagonism, Partial agonism, and Inverse agonism of various 5-HT receptor subtypes to modulate neurotransmission and downstream signaling pathways.

03

Biological functions

Signal transductionNeurotransmissionMood regulationVasoconstrictionPlatelet aggregationGastrointestinal motilityThermoregulationSleep-wake cycle regulation
04

Disease associations

DepressionAnxietySchizophreniaMigraineIrritable bowel syndromePulmonary arterial hypertensionObesityNauseaNeurodegenerative disease
05

Safety considerations

Serotonin syndromeCardiovascular valvulopathy (5-HT2B)Extrapyramidal symptomsSexual dysfunctionWeight gainQT prolongation
06

Interacting drugs

Sumatriptan

9 more in the full profile.

07

Biomarkers

5-Hydroxyindoleacetic acid (5-HIAA)Platelet serotonin levelsPET imaging of receptor density (e.g., [11C]WAY-100635)Serotonin transporter (SERT) occupancy

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