Eloísa Rubio-Beltrán, Alejandro Labastida-Ramírez, Kristian A Haanes, Antoon van den Bogaerdt, Ad J J C Bogers, Eric Zanelli, Laurent Meeus, A H Jan Danser, Michael R Gralinski, Peter B Senese, Kirk W Johnson, Joseph Kovalchin, Carlos M Villalón, Antoinette MaassenVanDenBrink
BACKGROUND AND PURPOSE: Triptans are 5-HT1B/1D receptor agonists (that also display 5-HT1F receptor affinity) with antimigraine action, contraindicated in patients with coronary artery disease due to their vasoconstrictor properties. Conversely, lasmiditan was developed as an antimigraine 5-HT1F receptor agonist. To assess the selectivity and cardiovascular effects of lasmiditan, we investigated the binding, functional activity, and in vitro/in vivo vascular effects of lasmiditan and compared it to sumatriptan...
December 2019: British Journal of Pharmacology