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Target intelligence / Profile preview
Serotonin Receptor 1A (5-HT1A)
- Target
- 5-HT1A
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The 5-HT1A receptor is a G protein-coupled receptor (GPCR) coupled to Gi/Go proteins. It is highly expressed in the central nervous system, particularly in the cerebral cortex, hippocampus, septum, amygdala, and raphe nuclei. It functions as both an autoreceptor on serotonin neurons and as a postsynaptic heteroreceptor. Upon activation by serotonin, it inhibits adenylyl cyclase, opens inwardly rectifying potassium channels, and inhibits voltage-gated calcium channels, leading to reduced neuronal excitability. It plays a role in mood regulation, anxiety, and the secretion of various hormones. It is a target for anxiolytic and antidepressant drugs.
- Other names
- Serotonin 1A receptorHTR1A (gene)
02
Mechanism of action
Agonism or modulation of 5-HT1A receptor activity; Inhibition of adenylyl cyclase/cAMP production; opening K+ channels; inhibition Ca²⁺ influx.
03
Biological functions
NeurotransmissionModulation of neuronal excitabilityEndocrine hormone secretionSignal transduction
04
Disease associations
Mood disordersAnxiety disordersDepression
05
Safety considerations
Delayed therapeutic onset of SSRIs due to autoreceptor activationPotential side effects associated with non-selective agonists
06
Interacting drugs
Buspirone
2 more in the full profile.
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