| Hazard Information | Back Directory | [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 ).
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| [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 |
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R&D Systems, Inc
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18003437475 18003437475 |
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www.rndsystems.com |
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