5-HT1A receptor

The 5 -HT1A receptor (abbr. 5 -HT1A ) is a protein in the cell membrane of vertebrate cells, mainly in the brain but also in peripheral nerve cells and in fetal lymphoid tissue. The receptor is localized pre-and postsynaptic mainly serves as serotonin in the synaptic gap sensor. Agonists at 5 -HT1A have potentially anxiolytic effect. The receptor belongs to the family of serotonin receptors. The corresponding gene is called Htr1a and is localized in humans on chromosome 5.


Of the 5-HT1A receptor is the most widely used serotonin receptor. It is found in the cerebral cortex, the hippocampus, the amygdala and in the raphe nuclei.

Medical importance

The 5 -HT1A receptor is the target in the treatment of anxiety disorders, blood pressure problems, psychosis and aggressive behavior disorders.

Signal transduction

The receptor is coupled to a blocking G- protein (Gi / Go). The binding of serotonin causes a decrease in intracellular concentration of cyclic adenosine monophosphate (cAMP ), and thereby for the inhibition of protein kinase A, then finally increasing the open probability of potassium channels. In addition, the L-type calcium channels are inhibited via the Go protein. These two mechanisms lead to a decreased release of serotonin.


Substances which bind to the 5 -HT1A receptor, for example: cannabidiol (CBD), ipsapirone, gepirone, buspirone, urapidil, tandospirone and 5-hydroxytryptamine ( Serotonin = 5- HT).


Substances which block the 5 -HT1A receptor among others: propranolol and dotarizine.