5-hydroxytryptamine receptor 1B, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2B (5-HT1B, 5-HT2A, 5-HT2B)

The 5-hydroxytryptamine (serotonin) receptors 1B, 2A, and 2B are members of the G protein-coupled receptor (GPCR) superfamily. These receptors are activated by the neurotransmitter serotonin, modulating a wide range of physiological functions in the central and peripheral nervous systems. 5-HT1B receptors primarily function as presynaptic inhibitory autoreceptors and heteroreceptors, participating in neurotransmitter release control and implicated in migraine treatment. 5-HT2A receptors play a central role in modulating mood, cognition, and perception, serving as the principal target for serotonergic psychedelic drugs and the site of action for many antipsychotics. 5-HT2B receptors, while less prominent in the central nervous system, are expressed in peripheral tissues (notably the heart) and are a target of concern regarding drug-induced valvular heart disease. All three subtypes are important pharmacological targets in psychiatry, neurology, and cardiology and are implicated in a variety of disease processes including mental health disorders, addiction, migraine, and cardiovascular risk.

Other names

Serotonin receptor 1BHTR1BSerotonin receptor 2AHTR2ASerotonin receptor 2BHTR2BSerotonin receptor subtypes

5-HT1B: Agonists inhibit neurotransmitter release via Gi/o signaling (decreasing cAMP) 5-HT2A/2B: Agonists activate Gq/11 signaling, increasing IP3/DAG and excitatory pathways Antagonists block serotonin-mediated activation, reducing various downstream effects (antipsychotic, anti-migraine, etc.) 5-HT2A: Partial agonism/biased agonism can lead to psychedelic or non-psychedelic outcomes, depending on downstream signaling pathway selectivity