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