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Papers of the Week

Papers: 17 Aug 2019 - 23 Aug 2019

Animal Studies, Human Studies, Pharmacology/Drug Development

2019 Dec

Br J Pharmacol



Characterization of binding, functional activity and contractile responses of the selective 5-HT receptor agonist lasmiditan.


Rubio-Beltrán E, Labastida-Ramírez A, Haanes KA, van den Bogaerdt A, Bogers A J, Zanelli E, Meeus L, Danser JAH, Gralinski MR, Senese PB, Johnson KW, Kovalchin J, Villalón CM, Maassen Van Den Brink A
Br J Pharmacol. 2019 Dec; 176(24):4681-4695.
PMID: 31418454.


Triptans are 5-HT receptor agonists (that also display 5-HT 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-HT 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.