Target intelligence / Profile preview

Serotonin receptor type 1A (5-HT1A receptor)

Target
5-HT1A receptor
Molecular classification
G protein-coupled receptor, Receptor, Neurotransmitter receptor
01

Overview

The serotonin receptor type 1A (5-HT1A receptor) is a G protein-coupled receptor (GPCR) that binds serotonin (5-hydroxytryptamine, 5-HT) and is encoded by the HTR1A gene[1][6]. It is the most widely distributed serotonin receptor in the brain, with high densities in the cerebral cortex, hippocampus, septum, amygdala, and raphe nuclei. The receptor functions as both a somatodendritic autoreceptor on serotonergic neurons—regulating serotonin release—and as a postsynaptic heteroreceptor on other neuron types, modulating mood, anxiety, cognition, and neuroendocrine function. Alterations in its expression or function have been directly linked to major depressive disorder, anxiety disorders, and other psychiatric conditions. Clinically, it is targeted by a range of drugs, including partial agonists (anxiolytics and antidepressants) and antagonists, and its gene polymorphisms serve as biomarkers for disease risk and therapeutic response[1][2][3][4][6].

Other names
5-hydroxytryptamine receptor 1AHTR1A5-HT1ASerotonin 1A receptorSerotonin-1A receptor
02

Mechanism of action

Agonist binding induces Gi protein coupling, reducing neuronal firing and cAMP production Partial agonists modulate receptor activity, resulting in antidepressant or anxiolytic effects Antagonists block serotonin binding, affecting serotonergic tone Regulation of presynaptic autoreceptors and postsynaptic heteroreceptors[1][3][4]

03

Biological functions

Signal transductionNeurotransmissionRegulation of neuronal firingRegulation of mood and anxietyControl of synaptic serotonin levels
04

Disease associations

Neuropsychiatric disordersDepressionAnxiety disordersBipolar disorderSchizophreniaOther neurodegenerative and mood disorders
05

Safety considerations

Risk of serotonin syndrome with pharmacological agonists or SSRIsAltered receptor function may increase risk of depression, anxiety, or suicidal ideationDrug–drug interactions with other serotonergic agentsChanges in receptor expression due to genetic polymorphisms[2][3]
06

Interacting drugs

Aripiprazole

9 more in the full profile.

07

Biomarkers

HTR1A C(-1019)G polymorphism (rs6295), associated with altered receptor expression and depressive risk[2]5-HT1A receptor binding potential as measured by PET for neuropsychiatric status or therapy response[2]

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