Role of Serotonin-2A Receptors in Pathophysiology and Treatment of Depression

This chapter aims to summarize the up-to-day evidence-based biomedical knowledge on serotonin-2A (5-HT2A) receptors and their role in pathophysiology and treatment of central nervous system (CNS) disorders, with a primary focus on depression. The first paragraph provides a brief introduction to serotonin (5-HT) system and 5-HT receptors, focusing on serotonin-2 (5-HT2) family and 5-HT2A receptor specifically. The second paragraph is focused on molecular genetics of 5-HT2A receptors, polymorphism of 5-HT2A receptor (5HT2AR) gene, 5HT2AR gene epigenetic mechanisms, such as DNA methylation, and post-translational modifications of 5HT2AR messenger ribonucleic acid (mRNA), such as alternative splicing. The molecular and cellular pharmacology and physiology of 5-HT2A receptors in normal and pathological conditions are discussed in the third paragraph. The 5-HT2A receptors-acting ligands are addresses. The fourth paragraph describes the role of 5-HT receptors in the interaction between 5-HT and other neurotransmitter systems in health and in CNS disorders. The fifth and the final paragraph specifically deals with the role of 5-HT2A receptor in pathophysiology and treatment of depression, focusing on the 5-HT2A receptor expressed in the hippocampus.