Selfotel

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CGS 19755 是一种选择性、竞争性 NMDA 拮抗剂，可抑制 [3H]-3-(2-羧基哌嗪-4-基)丙基-1-膦酸与 NMDA 型受体的结合，IC50 为 50 nM。

CGS 19755 is a selective, competitive NMDA antagonist that inhibits [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid binding to NMDA-type receptors with IC50 of 50 nM.(In Vitro):CGS 19755 reduces neuronal death concentration-dependently as assessed by phase-contrast microscopy and by measurement of LDH release into the bathing medium 20-24 h later with the mean (±SD) ED50 for CGS 19755 against NMDA toxicity of 25.4 ± 30.8 μM, determined from 6 experiments, each using 4 cultures per condition.(In Vivo):CGS 19755 blocks the harmaline-induced increase in cerebellar cyclic GMP levels (4 mg/kg i.p. 2 hr) and inhibits convulsions elicited by maximal electroshock in rats with ED50 of 3.8 mg/kg at 1 hr after i.p. administration and in mice with ED50 of 2.0 mg/kg at 0.5 hr after i.p. administration). P.O. administration of CGS 19755 by gavage has little or no effect in an experimental model of anxiety in rats while CGS 19755 significantly increases conflict responding within a relatively narrow dose range at the minimum effective dose of 1.73 mg/kg i.p..

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.

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).

CGS 19755 | Selfotel | LY-272541

Membrane Transporter/Ion Channel

NMDAR

RIPK1

——

——

110347-85-8

223.165

C7H14NO5P

>98% (HPLC)

In Vitro:?H2O : 10 mg/mL (44.81 mM)

OC(=O)[C@@H]1C[C@H](CP(O)(O)=O)CCN1

——

(-20℃)

With Ice Pack

≥ 2 years