riluzole

Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.

Riluzole-13C,15N2 is intended for use as an internal standard for the quantification of riluzole by GC- or LC-MS. Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals at an ED50 value of 4 mg/kg. Formulations containing riluzole have been explored as therapeutics for slowing disease progression of amyotrophic lateral sclerosis.

N-hydroxy Riluzole is a metabolite of the antiglutamatergic agent riluzole .1It is formed from riluzole predominantly by the cytochrome P450 (CYP) isoform CYP1A2 in human hepatic microsomes. 1.Sanderink, G.J., Bournique, B., Stevens, J., et al.Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitroJ. Pharmacol. Exp. Ther.282(3)1465-1472(1997)

Riluzole hydrochloride (PK 26124 hydrochloride) is an anticonvulsant compound belonging to the family of sodium channel blockers that inhibits GABA uptake.Riluzole hydrochloride is a sodium-glutamate antagonist with anticancer and neuroprotective activity and can be used to study amyotrophic lateral sclerosis and neurological disorders.

VGSCs-IN-1 is a potent VGSC inhibitor, a 2-piperazine analog of Riluzole that exhibits good blocking activity on Nav1.4.VGSCs-IN-1 can be used to study cellular excitability disorders.

Troriluzole is an orally active glutamate modulator with anticancer activity.Troriluzole enhances the expression of excitatory amino acid transporters located in glial cells and is used in the study of spinocerebellar ataxia, Alzheimer's disease, and generalized anxiety disorder (GAD).