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GYKI 52466 dihydrochloride

CAS No. : 2319722-40-0

MCE 站：GYKI 52466 dihydrochloride

产品活性：GYKI 52466 dihydrochloride 是一种有效的，选择性的，口服活性的和非竞争性的海藻酸盐 (kainate) 和 AMPA 活化电流拮抗剂，IC₅₀ 分别为 7.5 μM 和 11 μM。GYKI 52466 dihydrochloride 对 NMDA 或 γ-氨基丁酸反应无活性。GYKI 52466 dihydrochloride 是一种肌肉松弛剂和抗惊厥药，并具有良好的血脑屏障通透性。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

In Vitro: In kinetic experiments with kainate as the agonist, the GYKI 52466 binding and unbinding rates were 1.6 x 10⁵ M^-1 s^-1 and 3.2 s^-1, respectively. GYKI 52466 also suppresses non-NMDA receptor-mediated spontaneous synaptic currents via a postsynaptic action.

In Vivo: 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 seizure-susceptible 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.).
GYKI 52466 provides potent anticonvulsant protection against AMPA-induced seizures in Swiss mice. Maximal anticonvulsant protection is observed 5-15 min after the i.p. administration of GYKI 52466 in DBA/2 mice. The ED₅₀ values for the protection against AMPA-induced seizures by GYKI 52466 (15 min, i.p.) is 18.5 (11.5-29.5) μmol/kg.

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