5-HT1A receptor, 5-HT1B receptor, and 5-HT2C receptor (5-HT1A, 5-HT1B, 5-HT2C)

5-HT1A, 5-HT1B, and 5-HT2C receptors are subclasses of serotonin (5-hydroxytryptamine, 5-HT) receptors, which are G protein-coupled receptors distributed in both the central and peripheral nervous systems. The 5-HT1A and 5-HT1B receptors primarily couple to the Gi/Go class of G proteins, resulting in inhibition of adenylyl cyclase and decreased cellular cAMP, having mainly inhibitory modulatory functions in the nervous system. 5-HT2C receptors couple to Gq/11 proteins, activating phospholipase C and increasing IP3 and DAG, typically exerting excitatory effects. All three are involved in mood regulation, cognition, neurogenesis, appetite, pain perception, and vascular tone. They are targets for drugs treating depression, anxiety, migraine, and obesity, among other disorders. These receptors represent important therapeutic targets in neuropsychiatric and metabolic diseases, yet their wide distribution contributes to diverse side effects and therapeutic challenges.

Other names

Serotonin receptor 1A, 1B, 2C5-hydroxytryptamine receptor 1A, 1B, 2C5-HT1A, 5-HT1B, 5-HT2C

Agonism or antagonism at the receptor modulates downstream G protein signaling: 5-HT1A and 5-HT1B: Gi/Go-coupled, inhibit adenylyl cyclase and reduce cAMP levels; 5-HT2C: Gq/11-coupled, activates phospholipase C, increases IP3 and DAG. Regulation of neurotransmitter (serotonin) release (autoreceptor and heteroreceptor effects). Modulation of neuronal excitability and neurogenesis.