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Selfotel

CAS No. : 110347-85-8

MCE 站：Selfotel

产品活性：Selfotel (CGS 19755) 是选择性的、竞争性的 (NMDA) 拮抗剂，其抑制 [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid 结合到 NMDA 型受体的 IC₅₀ 值为 50 nM。

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

作用靶点：iGluR

In Vitro: Selfotel (CGS 19755) results in a concentration-dependent reduction in neuronal death as assessed by phase-contrast microscopy ａnd by measurement of LDH release into the bathing medium 20-24 h later. The mean (±SD) ED₅₀ for CGS 19755 against NMDA toxicity is 25.4 ± 30.8 μM, determined from 6 experiments, each using 4 cultures per condition.

In Vivo: Selfotel (CGS 19755) administered p.o. by gavage has little or no effect in these test procedures. In an experimental model of anxiety in rats.
Selfotel (CGS 19755) significantly increases conflict responding within a relatively narrow dose range (minimum effective dose, 1.73 mg/kg i.p.).
Selfotel (CGS 19755) blocks the harmaline-induced increase in cerebellar cyclic GMP levels at a dose of 4 mg/kg i.p. with duration of action exceeding 2 hr.
Selfotel (CGS 19755) inhibits convulsions elicited by maximal electroshock in rat (ED₅₀ = 3.8 mg/kg i.p. 1 hr after administration) ａnd in mouse (ED₅₀ = 2.0 mg/kg i.p. 0.5 hr after administration).

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