Eletriptan
Based on 2 publication(s) in Google Scholar
Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 143322-58-1
- Fòrmula: C22H26N2O2S
- Peso molecular:382.52
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Eletriptan
MoreVer todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
5-HT1B Receptor |
5-HT1D Receptor |
5-HT1B Receptor 8.0 (pKi) |
5-HT1D Receptor 8.9 (pKi) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 143322-58-1
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Peso molecular 382.52
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Fòrmula C22H26N2O2S
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SMILES
CN1[C@@H](CC2=CNC3=CC=C(CCS(C4=CC=CC=C4)(=O)=O)C=C32)CCC1
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Synonyms
UK-116044
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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J Headache Pain
Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action. [Abstract]2024 Oct 30;25(1):187. PMID: 39478486 -
Protocolo
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureza y Documentación
Referencias
[1]. McCormack PL, Keating GM. Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2006;66(8):1129-49. [Content Brief]
[2]. Willems E, et al. Porcine carotid vascular effects of eletriptan (UK-116,044): a new 5-HT1B/1D receptor agonist with anti-migraine activity. Naunyn Schmiedebergs Arch Pharmacol. 1998 Aug;358(2):212-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)