Target intelligence / Profile preview

Serotonin 1F Receptor (5-HT1F)

Target: 5-HT1F
Molecular classification: G protein-coupled receptor, Receptor

Overview

The serotonin 1F receptor (5-HT1F, HTR1F) is a G protein-coupled receptor that binds serotonin. It is expressed in the central nervous system, particularly in the cortex, hippocampus, and trigeminal ganglia, as well as in some peripheral tissues. Its primary function involves modulation of neuronal activity and inhibition of trigeminal impulses implicated in migraine pain transmission. Unlike other serotonin receptor subtypes, activation of the serotonin ₁𝐹 receptor does not cause vasoconstriction, making it a target for migraine therapies without cardiovascular side effects. Lasmiditan is a selective agonist approved for the acute treatment of migraine.

Other names: HTR1F5-HT-1F5-HT1FMR77HTR1EL5-hydroxytryptamine receptor 1F

Mechanism of action

Selective activation of the serotonin ₁𝐹 receptor inhibits pain pathways without causing blood vessel constriction.

Biological functions

Signal transductionModulation of neuronal activityInhibition of trigeminal impulses

Disease associations

Migraine

Safety considerations

Potential cardiovascular side effects with non-selective agonists (e.g., triptans)Limited data on long-term safety of selective 5-HT1F agonists

Interacting drugs

Lasmiditan

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