lasmiditan hydrochloride

  • Chemical Properties
CAS No. 613677-28-4 Cat. No. BCP17274
Name lasmiditan hydrochloride
Synonyms COL 144 hydrochloride;LY 573144 hydrochloride;COL-144 hydrochloride; LY-573144 hydrochloride;COL144 hydrochloride;LY573144 hydrochloride;
Formula C19H19ClF3N3O2 M. Wt 413.82
  • Biological Activity
Description in vitro: In vitro binding studies Lasmiditan showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor, compared with K(i) values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan show 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. Unlike the 5-HT(1B/1D) receptor agonist sumatriptan, lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 μM. in vivo: In two rodent models of migraine, oral administration of lasmiditan potently inhibited markers associated with electrical stimulation of the trigeminal ganglion (dural plasma protein extravasation, and induction of the immediate early gene c-Fos in the trigeminal nucleus caudalis).
Pathways Neuro Signaling Pathway GPCR/G Protein 
Targets 5 HT Receptor/Serotonin Receptor 

Structure

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