Lasmiditan mechanism of action - review of a selective 5-HT1F agonist

The Journal of Headache and Pain
David B ClemowAndrew M Blumenfeld

Abstract

Migraine is a leading cause of disability worldwide, but it is still underdiagnosed and undertreated. Research on the pathophysiology of this neurological disease led to the discovery that calcitonin gene-related peptide (CGRP) is a key neuropeptide involved in pain signaling during a migraine attack. CGRP-mediated neuronal sensitization and glutamate-based second- and third-order neuronal signaling may be an important component involved in migraine pain. The activation of several serotonergic receptor subtypes can block the release of CGRP, other neuropeptides, and neurotransmitters, and can relieve the symptoms of migraine. Triptans were the first therapeutics developed for the treatment of migraine, working through serotonin 5-HT1B/1D receptors. The discovery that the serotonin 1F (5-HT1F) receptor was expressed in the human trigeminal ganglion suggested that this receptor subtype may have a role in the treatment of migraine. The 5-HT1F receptor is found on terminals and cell bodies of trigeminal ganglion neurons and can modulate the release of CGRP from these nerves. Unlike 5-HT1B receptors, the activation of 5-HT1F receptors does not cause vasoconstriction.The potency of different serotonergic agonists towards 5-HT1F was c...Continue Reading

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Citations

Jan 7, 2021·Therapeutic Advances in Neurological Disorders·Jasper MecklenburgUwe Reuter
Feb 21, 2021·Clinical Therapeutics·Anna Ferrari, Cecilia Rustichelli
Mar 19, 2021·Postgraduate Medicine·David B ClemowJessica Ailani
Apr 1, 2021·Current Medical Research and Opinion·Mario F P PeresDeborah I Friedman
Apr 4, 2021·International Journal of Molecular Sciences·Jinsha LiuSepideh Afshar
Apr 13, 2021·Expert Opinion on Pharmacotherapy·Masaru TanakaLászló Vécsei
May 1, 2021·Journal of Clinical Medicine·Matilde CapiPaolo Martelletti
Jun 1, 2021·Frontiers in Neuroscience·Athanasios LourbopoulosConstantinos Pantos
Jun 22, 2021·Expert Review of Pharmacoeconomics & Outcomes Research·Karissa JohnstonJames Moren
Jan 28, 2022·The Journal of Headache and Pain·Astrid WiggersMessoud Ashina

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