Lasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity.
Storage Temp
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Action Type
AGONIST
Mechanism of action
Serotonin 1f (5-HT1f) receptor agonist
Product Description
Information
Lasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective5-HT(1F) receptoragonist (Ki=2.21 nM) without vasoconstrictor activity.
Targets
5-HT(1F) (Cell-free assay) 2.21 nM(Ki)
In vitro
Lasmiditan shows higher selectivity for the 5-HT(1F) receptor relative to other 5-HT(1) receptor subtypes than the first generation 5-HT(1F) receptor agonist LY334370.
In vivo
Lasmiditan is orally active in two in vivo models of migraine that involve electrical stimulation of the trigeminal ganglion. After oral administration, lasmiditan potently decreases dural plasma protein extravasation and the number of c-fos positive cells in the trigeminal nucleus caudalis at a dose of 3 mg/kg.
This compound belongs to the class of organic compounds known as 4-halobenzoic acids and derivatives. These are benzoic acids or derivatives carrying a halogen atom at the 4-position of the benzene ring.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
