The 5-Hydroxytryptamine receptor 1A (5-HT1A) is Gi-coupled GPCRs expressed in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucelus, with lesser amounts in the basal ganglia and thalamus. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal and appetite. 5-HT1A ligands may prove to be therapeutic in the trea™ent of various disorders such as depression, anxiety, and schizophrenia.