ChemicalBook CAS DataBase List 2319722-40-0

2319722-40-0

Name	GYKI 52466 dihydrochloride
CAS	2319722-40-0
Molecular Formula	C17H16ClN3O2
MDL Number	MFCD03453303
Molecular Weight	329.78
MOL File	2319722-40-0.mol

Chemical Properties

solubility	Soluble to 50 mM in DMSO and to 10 mM in water
form	Solid
color	Yellow to orange

Hazard Information

Uses

GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research[1][2].

Biological Activity

GYKI 52466 dihydrochloride is a selective noncompetitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >50 μM for AMPA-, kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant. Has anti-proliferative effects in transformed cells.

in vivo

GYKI 52466 (intraperitoneal injection; 1.76-13.2 mg/kg; once) treatment provides potent anticonvulsant protection against sound-induced seizures in DBA/2 mice^[2].

Animal Model:	Male and female DBA/2 mice tested for sound-induced seizure responses^[2]
Dosage:	1.76-13.2 mg/kg
Administration:	Intraperitoneal injection; 1.76-13.2 mg/kg; once
Result:	Observed Maximal anticonvulsant protection after the i.p. treatment (5-15 min ).

IC 50

Kainate Receptor: 11 μM (IC₅₀)

storage

Store at -20°C

References

[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. DOI:10.1016/0896-6273(93)90241-i
[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. DOI:10.1016/0920-1211(91)90018-b

Supplier

Related Products

Send Inquriy