Target intelligence / Profile preview

5-hydroxytryptamine receptor 1 (5-HT1 receptor) (5-HT1 receptor)

Target
5-HT1 receptor
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

The **5-hydroxytryptamine receptor 1 (5-HT1 receptor) family** comprises a group of G protein-coupled receptors that mediate the inhibitory actions of serotonin (5-HT) in the central and peripheral nervous systems by coupling primarily to Gi/o proteins, thereby inhibiting adenylyl cyclase and decreasing cAMP levels. Individual family members — including 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F — have distinct expression patterns and functional roles in modulating behavior, sensation, cognition, and vascular tone, and are targeted by various psychiatric and antimigraine drugs. "Serotonin receptor 1" should be clarified to a specific subtype for more precise discussion.

Other names
Serotonin receptor 15-HT15-HT1 receptor family5-hydroxytryptamine receptor 1 familyHTR1 (gene family)
02

Mechanism of action

Agonists: Activate Gi/o protein-coupled pathways, leading to inhibition of adenylyl cyclase activity, reducing cyclic AMP (cAMP) production, and causing neuronal hyperpolarization (opening of K+ channels by 5-HT1A, for example). Antagonists: Block receptor-mediated inhibition, can modulate neurotransmitter release.

03

Biological functions

Signal transductionModulation of neurotransmissionRegulation of neuronal inhibition/hyperpolarizationModulation of mood, cognition, and various physiological responses
04

Disease associations

Neuropsychiatric disorders (depression, anxiety, schizophrenia)MigrainePainNeurodegenerative disease (emerging evidence)Cancer (emerging evidence for select subtypes)
05

Safety considerations

CNS side effects (e.g., dizziness, sleep disturbances, cognitive effects)Cardiovascular risk (triptans and vasoconstriction via 5-HT1B)Off-target effects due to poor selectivity among subtypes
06

Interacting drugs

Triptans (e.g., sumatriptan), target 5-HT1B/1D for migraine

4 more in the full profile.

07

Biomarkers

Expression levels of 5-HT1A (for some neuropsychiatric conditions, PET imaging ligand use)No routinely used clinical biomarkers for the general 5-HT1 receptor family; mostly research tools

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