The working lives of neuronal 5-HT2A receptors from the outside in

Abstract

5-HT2A receptors have been shown to play critical roles in regulating neuronal signalling networks and brain plasticity. They have become important targets for the treatment of resistant forms of depression and other neurological disorders, such as anxiety and PTSD. Like many G proteincoupled receptors (GPCRs), signalling downstream of the 5-HT2A depends on where the receptor is in the cell. Events and signalling pathways modulated by the cell surface pool of receptors may be distinct from those regulated by an internal pool of receptors. In this review, we attempt to parse out how the cell organizes and regulates this location bias and explore attempts to target the distinct receptor pools pharmacologically.