CGS 19755 是一种选择性的、竞争性的(NMDA)拮抗剂，能够抑制 [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid 结合到 NMDA 型受体的IC50值为 50 nM。

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.

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[1].

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)[1]. 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.[2].

110347-85-8

C7H14NO5P

223.16

LY-272541;CGS 19755;塞福太

H2O:<5 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years