110347-85-8

110347-85-8 structure

Name: CGS 19755
Chemical Name: cis-4-(phosphonomethyl)-2-piperidinecarboxylic acid
CAS Number: 110347-85-8
Molecular Formula: C₇H₁₄NO₅P
Molecular Weight: 223.16400
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2018-09-01 07:23:01
Modify Date: 2024-01-02 08:58:37
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].

Name	cis-4-(phosphonomethyl)-2-piperidinecarboxylic acid
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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> iGluR Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
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	[1]. D A Bennett, et al. Behavioral pharmacological profile of CGS 19755, a competitive antagonist at N-methyl-D-aspartate receptors. J Pharmacol Exp Ther. 1989 Aug;250(2):454-60. [2]. J Lehmann, et al. CGS 19755, a selective and competitive N-methyl-D-aspartate-type excitatory amino acid receptor antagonist. J Pharmacol Exp Ther. 1988 Jul;246(1):65-75. [3]. M A Pérez-Pinzón, et al. Correlation of CGS 19755 neuroprotection against in vitro excitotoxicity and focal cerebral ischemia. J Cereb Blood Flow Metab. 1995 Sep;15(5):865-76.

Density	1.440±0.06 g/cm3(Predicted)
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

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