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The Serotonin Receptor 5HT1A is a Gi/o-coupled GPCR encoded by HTR1A with widespread CNS distribution. It functions both presynaptically as an autoreceptor regulating serotonergic tone via negative feedback mechanisms—and postsynaptically modulating neuronal excitability across multiple brain regions involved in emotion/mood regulation. Its pharmacological targeting underlies several therapeutic strategies for mood/anxiety disorders due to its central role in emotional balance.
Agonists, partial agonists, or antagonists modulate the activity of the 5-HT1A receptor, influencing downstream signaling pathways involving adenylyl cyclase inhibition, potassium channel activation, and calcium channel inactivation. This leads to changes in neuronal excitability and serotonergic neurotransmission.
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