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The serotonin 5-HT1A receptor is a subtype of serotonin receptors belonging to the G protein-coupled receptor (GPCR) family. It is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It functions both as an autoreceptor on serotonergic neurons, inhibiting serotonin release, and as a heteroreceptor on postsynaptic neurons, modulating neuronal excitability. Activation of the 5-HT1A receptor leads to hyperpolarization of neurons and affects various physiological processes, including mood regulation and hormone secretion. It is a key target for anxiolytic and antidepressant drugs.
Agonists bind to the 5-HT1A receptor, leading to activation of Gi/Go proteins. This results in inhibition of adenylyl cyclase, reduction of cAMP levels, opening of inwardly rectifying potassium channels (GIRK), and hyperpolarization of the neuron. Autoreceptor activation reduces serotonin release, while postsynaptic activation modulates neuronal excitability.
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