912574-69-7

912574-69-7 structure

Name: Selurampanel
Chemical Name: N-[6-(2-methylpyrazol-3-yl)-2,4-dioxo-7-propan-2-yl-1H-quinazolin-3-yl]methanesulfonamide
CAS Number: 912574-69-7
Molecular Formula: C₁₆H₁₉N₅O₄S
Molecular Weight: 377.42
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2018-10-07 17:42:24
Modify Date: 2024-04-03 17:45:54
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].

Name	N-[6-(2-methylpyrazol-3-yl)-2,4-dioxo-7-propan-2-yl-1H-quinazolin-3-yl]methanesulfonamide
Synonyms	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]

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.