5-hydroxytryptamine receptor 1F (5-HT1F) (5-HT1F)

The 5-hydroxytryptamine receptor 1F (5-HT1F) is a member of the G protein-coupled receptor (GPCR) family that mediates the effects of serotonin in the central and peripheral nervous systems [7, 9]. It is notably expressed in the trigeminal ganglion and the trigeminal nucleus caudalis, where it plays a critical role in modulating pain signaling pathways [4, 11]. Unlike other serotonin receptors like 5-HT1B, the 5-HT1F receptor is not found on vascular smooth muscle, meaning its activation does not induce vasoconstriction [1, 3]. This unique profile led to the development of "ditans," such as lasmiditan, which are selective 5-HT1F agonists used for the acute treatment of migraine [8, 16]. By activating 5-HT1F receptors, these drugs inhibit the release of pro-inflammatory neuropeptides, including calcitonin gene-related peptide (CGRP) and glutamate, effectively aborting migraine attacks without the cardiovascular risks associated with traditional triptans [4, 15].

Other names

HTR1FSerotonin receptor 1F5-HT1F receptorHTR1EL5-HT1E beta

Selective agonism of the 5-HT1F receptor to inhibit trigeminal nerve activation and the release of pro-inflammatory neuropeptides like CGRP and glutamate without inducing vasoconstriction.