Name | cis-4-(phosphonomethyl)-2-piperidinecarboxylic acid |
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Synonyms |
cis-4-phosphonomethyl-2-piperidine-carboxylic acid
Selfotel |
Description | Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM[1][2]. |
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Related Catalog | |
Target |
IC50: 50 nM (the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors)[2]. |
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[2]. |
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[1]. Selfotel (CGS 19755) significantly increases conflict responding within a relatively narrow dose range (minimum effective dose, 1.73 mg/kg i.p.)[1]. 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[2]. 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)[2]. |
References |
Density | 1.440±0.06 g/cm3(Predicted) |
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Boiling Point | 508.6±60.0 °C(Predicted) |
Melting Point | 290-292 °C |
Molecular Formula | C7H14NO5P |
Molecular Weight | 223.16400 |
Exact Mass | 223.06100 |
PSA | 116.67000 |