Review of antidepressants in clinic and active ingredients of traditional Chinese medicine targeting 5-HT1A receptors

Abstract

Serotonin, which also named as 5-hydroxytryptamine (5-HT), is a neurotransmitter, which plays significant roles in a wide range of physiological and pathological processes. Depression is a complex disease that involves numerous factors, increasing evidences have showed that the level of 5-HT was lower in depressed patients and the administration of some selective serotonin re-uptake inhibitors exhibited antidepressant effects. The 5-HT1A receptor is a key protein in the brain serotonin system, modulating the release of 5-HT and other neurotransmitters. Behavioral and molecular biological studies have demonstrated that the differences of 5-HT1A receptor regulation was connected with depression and the responses to antidepressants. In this review, the authors will introduce the structure and function of 5-HT1A receptor and summarize some antidepressants targeting 5-HT1A receptor, including 5-HT1A receptor agonists and antagonists in a clinic, active ingredients of traditional Chinese medicine. And we found the major of drugs by targeting 5-HT1A receptor on the market or in clinical trials mostly have the similar functional groups, such as piperazine, piperidine, and pyrimidine. There are also some literatures found that these functional groups may be the site produce activity. So, we hope that it may provide basis and references for the research of the clinical drugs for depression.

Keywords: 5-HT1A receptor; Active ingredients of traditional Chinese medicine; Agonist; Antagonist; Depression.