5-HT5 Receptor Antagonists Small Molecules and Peptides

Serotonin 5-ht₅ receptors are G-protein-coupled receptors that preferentially couple to G_s and promote cAMP formation. Two 5-ht₅ receptor subtypes (5-ht_5a and 5-ht_5b) have been found in rodents and humans. mRNA for the human ortholog of the 5-ht_5a receptor has been found in human cerebral cortex, hippocampus, and cerebellar tissue, and in vitro studies have shown functional G protein coupling of the 5-ht_5a receptor upon ligand binding. A potential role in mood, cognitive function, circadian rhythm and shizophrenia has been suggested for the 5-ht_5a receptor. A functional transcript of the 5-ht_5b receptor has not yet been identified in humans.