GYKI 52466

GYKI 52466 is a potent antagonist of kainate- and AMPA-activated currents (IC50 values, 7.5 and 11 μM, respectively), GYKI 52466 can be used for the research of neurological disorders, such as Parkinson's disease[1].

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

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

GYKI 52466 (1.76-13.2 mg/kg; male and female DBA/2 mice; intraperitoneal injection) treatment provides potent anticonvulsant protection against sound-induced seizures in DBA/2 mice. The ED50 value at 15 min for the protection against sound-induced seizures in DBA/2 mice is 13.7 (11.5-16.5) μmol/kg (GYKI 52466, i.p.), The ED50 value for the protection against AMPA-induced seizures by GYKI 52466 (15 min i.p.) is 18.5 (11.5–29.5) μmol/kg[2]. Animal Model: Animal model: male and female DBA/2 mice tested for sound-induced seizure responses[2] Dosage: 1.76-13.2 mg/kg (6-45 μmol/kg) Administration: Intraperitoneal injection; 1.76-13.2 mg/kg (6-45 μmol/kg); once; 5 min, 15 min, 30 min Result: Observed Maximal anticonvulsant protection after the i.p. administration (5–15 min ) of GYKI 52466 in DBA/2 mice.

[1]. S D Donevan, et al. GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses. Neuron. 1993 Jan;10(1):51-9.

[2]. A G Chapman, et al. The anticonvulsant effect of the non-NMDA antagonists, NBQX and GYKI 52466, in mice. Epilepsy Res. 1991 Jul;9(2):92-6.