GYKI53655 hydrochloride is an antagonist of α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA).

GYKI53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons (IC50 value of 1.5±0.1 μM). GYKI53655 hydrochloride inhibits α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 μM)-induced responses (IC50: 5.9±0.1 μM). GYKI53655 hydrochloride inhibits AMPA (10 μM) responses in recombinant G1uR4 expressing HEK293 cells (IC50: 4.6±0.4 μM). GYKI53655 hydrochloride produces only small inhibitions of kainate-induced currents at 30 μM and inhibits kainate-induced currents at a concentration of 100 μM by 12±2 (n=4) and 18±4 (n=4), respectively. Using 3 μM cyclothiazide the inhibition produced by GYKI53655 hydrochloride is 79±2% (n=4 cells) [1].

The dose-dependence of GYKI53655 hydrochloride (2 to 8 mg/kg) in depressing responses to AMPA. Tonic fit and death are completely prevented by GYKI53655 hydrochloride at a dose of over 5.0 mg/kg (ED50: 2.2 mg/kg i.p). GYKI53655 hydrochloride (4 mg/kg) is found to have a short-lasting depressant effect on neuronal responses to iontophoretic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), with a half-recovery time of approximately 7 min. GYKI53655 hydrochloride (4 and 8 mg/kg) substantially depresses or completely abolishes AMPA responses. At the highest doses tested, GYKI53655 hydrochloride decreases AMPA responses to a comparable degree[2]. The maximal effects of GYKI53655 hydrochloride last 3 h then the exit inhibition effect of GYKI53655 hydrochloride falls to 20% 1 h later[3].

143692-48-2

C19H21ClN4O3

388.85

GYKI53655 hydrochloride

DMSO:160 mg/mL (411.47 mM)
H2O:8 mg/mL (20.57 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years