Target intelligence / Profile preview

Serotonin 5-HT1F Receptor (5-HT1F)

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

Overview

The serotonin 5-HT1F receptor is a G protein-coupled receptor that binds serotonin. It mediates inhibitory neurotransmission by coupling to Gi/Go proteins, leading to inhibition of adenylyl cyclase and decreased cAMP levels. Activation does not cause vasoconstriction, making it a target for migraine therapy, particularly for patients with cardiovascular risk factors. Selective agonists (ditans) like lasmiditan are used for acute migraine treatment.

Other names: 5-hydroxytryptamine receptor 1FHTR1ELMR77

Mechanism of action

Activation leads to reduced neuronal excitability via inhibition of adenylyl cyclase/cAMP pathway.

Biological functions

Inhibitory neurotransmissionInhibition of adenylyl cyclase activityRegulation of glutamate release

Disease associations

MigrainePain modulation

Safety considerations

Cardiovascular risk (triptans)Vascular safety (compared to older antimigraine drugs)

Interacting drugs

Lasmiditan

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