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The 5-hydroxytryptamine 1A receptor (5-HT1A receptor) is a subtype of serotonin receptors encoded by the HTR1A gene. It is a G protein-coupled receptor (GPCR) coupled to Gi protein. When activated, it mediates hyperpolarization and reduces the firing rate of the postsynaptic neuron by decreasing cellular cAMP levels. It is the most widespread 5-HT receptor, found in high densities in areas like the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus. It also interacts with BDNF and forms heterodimers with other receptors. Several genetic variations in the HTR1A gene have been studied, particularly in relation to psychiatric disorders, although definitive results are lacking.
As a Gi/Go coupled receptor, the 5-HT1A receptor functions by decreasing cellular levels of cAMP, producing an inhibitory potential. At sufficiently high doses, 5-HT1A receptor agonists can bypass autoreceptor-mediated inhibition and directly activate postsynaptic receptors.
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