Selurampanel

Names

[ Name ]:
Selurampanel

[Synonym ]:
UNII-7WG1MR7DAR
Selurampanel
Methanesulfonamide,N-(1,4-dihydro-7-(1-methylethyl)-6-(1-methyl-1H-pyrazol-5-yl)-2,4-dioxo-3(2H)-quinazolinyl)
Selurampanel [INN]

Biological Activity

[Description]:

Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[In Vivo]

Selurampanel (Compound 1S) potently and dose-dependently antagonizes maximal electroshock seizure (MES)-induced generalized tonic-clonic seizures in mice with an ED50 value around 7 mg/kg after 1 h pre-treatment[1]. In a study with a 3 mg/kg i.v. dose, a mouse plasma half-life of 3.3 h is determined, with a moderate volume of distribution (Vdss=1.3 L/kg) and a low clearance of 5.4 mL/min▪kg[1].

[References]

[1]. David Orain, et al. Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist. ChemMedChem. 2017 Feb 3;12(3):197-201.

[2]. Edward Faught, et al. BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy. Expert Opin Investig Drugs. 2014 Jan;23(1):107-13.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₁₉N₅O₄S

[ Molecular Weight ]:
377.42

[ Exact Mass ]:
377.11600

[ PSA ]:
127.49000

[ LogP ]:
2.28290

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.