Lasmiditan - CAS 439239-90-4
Catalog number: B0084-459175
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H18F3N3O2
Molecular Weight:
377.36
COA:
Inquire
Targets:
5-HT Receptor
Description:
Lasmiditan is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM) for the treatment of acute migraine.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-459175 300 mg $299 In stock
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Purity:
≥98 %
Related CAS:
439239-90-4 (Free base); 613677-28-4 (HCl)
Appearance:
Solid powder
Synonyms:
2,4,6-Trifluoro-N-(6-((1-methylpiperidine-4-yl)carbonyl)pyridin-2-yl)benzamide; COL-144; COL144; COL 144; LY573144; LY-573144; LY 573144; Lasmiditan
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
5-HT1F receptor agonist
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
XEDHVZKDSYZQBF-UHFFFAOYSA-N
InChI:
1S/C19H18F3N3O2/c1-25-7-5-11(6-8-25)18(26)15-3-2-4-16(23-15)24-19(27)17-13(21)9-12(20)10-14(17)22/h2-4,9-11H,5-8H2,1H3,(H,23,24,27)
Canonical SMILES:
O=C(NC1=NC(C(C2CCN(C)CC2)=O)=CC=C1)C3=C(F)C=C(F)C=C3F
Current Developer:
CoLucid Pharmaceuticals
1.Lasmiditan for the treatment of migraine.
Capi M;de Andrés F;Lionetto L;Gentile G;Cipolla F;Negro A;Borro M;Martelletti P;Curto M Expert Opin Investig Drugs. 2017 Feb;26(2):227-234. doi: 10.1080/13543784.2017.1280457.
Migraine is one of the most common diseases in the world, with high economical and subjective burden. Migraine acute therapy is nowadays based on specific and non-specific drugs but up to 40% of episodic migraineurs still have unmet treatment needs and over 35% do not benefit from triptans administration. Serotonin-1F receptors have been identified in trigeminal system and became an ideal target for anti-migraine drug development as potential trigeminal neural inhibitors. Lasmiditan, a novel serotonin1F receptor agonist, showed specific affinity in vitro for the receptor without any vasoconstrictive action and inhibited markers associated with electrical stimulation of trigeminal ganglion in migraine animal models. Areas covered: This article reviews both preclinical and clinical studies on lasmiditan as a potential acute therapy for migraine, as well as pharmacokinetic and pharmacodynamic features. It also summarizes safety and tolerability data gathered in the various human studies. Expert opinion: The absence of vasoconstrictive effects makes lasmiditan a promising novel migraine acute therapy. Although preclinical and Phase I and II studies established a significant efficacy, the limited knowledge about pharmacokinetics and metabolism, the high rate of non-serious central nervous system side effects and the lack of larger studies remain still a matter of concern that should be addressed in future studies.
2.Emerging treatments for the primary headache disorders.
Schuster NM;Vollbracht S;Rapoport AM Neurol Sci. 2015 May;36 Suppl 1:109-13. doi: 10.1007/s10072-015-2133-1.
Migraine and cluster headache are common, episodic, often chronic and disabling disorders of the brain. Although there are many standard treatment techniques, none are ideal. This article reviews various novel pharmacologic and device-related treatments for migraine and cluster headache. Emphasis is given to recent advances in the development of monoclonal antibodies (mAbs) targeting calcitonin gene-related peptide (CGRP) and its receptor, including promising results from phase 2 trials studying the safety and efficacy of LY2951742, ALD403 and TEV-48125, three anti-CGRP mAbs. Other new pharmacologic treatments discussed include the 5-HT1F receptor agonist lasmiditan and glial cell modulator ibudilast. Also reviewed is neuromodulation for migraine and cluster headache, including promising recent results of randomized controlled trials studying sphenopalatine ganglion stimulation, trigeminal nerve stimulation, transcutaneous vagus nerve stimulation, and transcranial magnetic stimulation. Finally, we discuss patch, inhaled, and intranasal methods of triptan and dihydroergotamine delivery.
3.Emerging treatment for chronic migraine and refractory chronic migraine.
Lionetto L;Negro A;Palmisani S;Gentile G;Del Fiore MR;Mercieri M;Simmaco M;Smith T;Al-Kaisy A;Arcioni R;Martelletti P Expert Opin Emerg Drugs. 2012 Sep;17(3):393-406. doi: 10.1517/14728214.2012.709846. Epub 2012 Aug 3.
INTRODUCTION: ;Chronic migraine (CM), the suffering of 15 or more headache days with at least 8 of these migraine days, afflicts 1.3% - 5.1% of the global population. CM is the most common disorder faced by experts in tertiary headache centers. When resistant to conventional medical treatment and prophylactic medication this condition is known as refractory chronic migraine (RCM). RCM is one of the greatest challenges in headache medicine.;AREAS COVERED: ;State-of-the-art and future medical treatments of chronic migraine include: OnabotulinumtoxinA, antiepileptic drugs (Levetiracetam, Magnesium valproate hydrate, Lacosamide, BGG-492), 5-HT agonists (Lasmiditan, NXN-188, novel delivery systems of Sumatriptan, a well-established drug treatment for acute migraine), CGRP receptor antagonists (BMS-927711), ML-1 agonists (Ramelteon), orexin receptor antagonist (MK-6096), plant-derived compound (LLL-2011) and other multitarget drugs such as Tezampanel, Tonabersat, intranasal carbon dioxide and BOL-148. The role for neuromodulation, the application of targeted electrical stimulation, will be examined.;EXPERT OPINION: ;Medication overuse headache (MOH) is now recognized to be a major factor in many cases of both chronic and refractory chronic migraine.
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CAS 439239-90-4 Lasmiditan

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