GYKI 53655 hydrochloride

Research use only, not for human use.

GYKI 53655 hydrochloride (LY300168 hydrochloride) is an antagonist of AMPA and is used in the study of neurological disorders.

GYKI 53655 (LY300168) hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.

GYKI 53655 (LY300168) hydrochloride inhibits α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 μM)-induced responses with IC50 value of 5.9±0.1 μM. GYKI 53655 hydrochloride inhibits AMPA (10 μM) responses in recombinant G1uR4 expressing HEK293 cells with IC50 value of4.6±0.4 μM. Using 3 μM cyclothiazide the inhibition produced by GYKI 53655 hydrochloride is 79±2%(n=4 cells). GYKI 53655 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. GYKI 53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons with an IC50 value of 1.5±0.1 μM.

GYKI 53655 hydrochloride (4 mg/kg) is found to have a short-lasting depressant effect on neuronal responses to iontophoreticα-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), with a half-recovery time of approximately 7 min. GYKI 53655 hydrochloride (4 and 8 mg/kg) substantially depresses or completely abolishes AMPA responses. Results demonstrate the dose-dependence of GYKI 53655 hydrochloride (2 to 8 mg/kg) in depressing responses to AMPA. At the highest doses tested, GYKI 53655 hydrochloride reduces AMPA responses to a comparable degree. Tonic fit and death are completely prevented by GYKI 53655 hydrochloride at dose over 5.0 mg/kg. The ED50 value of GYKI 53655 hydrochloride is 2.2 mg/kg i.p. The maximal effects of GYKI 53655 hydrochloride lasts 3 h then the exit inhibition effect of GYKI 53655 hydrochloride falls to 20% 1 h later.

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Neuroscience

GluR

GluR

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143692-48-2

388.85

C19H21ClN4O3

>98% (HPLC)

In Vitro:?DMSO : ≥ 160 mg/mL (411.47 mM)

Cl.CNC(=O)N1N=C(c2ccc(N)cc2)c2cc3OCOc3cc2CC1C

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(-20℃)

With Ice Pack

≥ 2 years