CGS 19755 - CAS 110347-85-8
Category: Inhibitor
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NMDA Receptor
CGS 19755 is a potent and competitive NMDA receptor antagonist with anticonvulsant, anxiolytic, analgesic and neuroprotective activity.
Brife Description:
NMDA receptor antagonist
CGS-19755; CGS 19755; CGS19755; CPDD 0027; CPDD-0027; CPDD0027; Selfotel; cis-4-[Phosphomethyl]-piperidine-2-carboxylic acid
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1.Glutamate receptor antagonists inhibit calpain-mediated cytoskeletal proteolysis in focal cerebral ischemia.
Minger SL;Geddes JW;Holtz ML;Craddock SD;Whiteheart SW;Siman RG;Pettigrew LC Brain Res. 1998 Nov 9;810(1-2):181-99.
Excitatory amino acids may promote microtubular proteolysis observed in ischemic neuronal degeneration by calcium-mediated activation of calpain, a neutral protease. We tested this hypothesis in an animal model of focal cerebral ischemia without reperfusion. Spontaneously hypertensive rats were treated with 2, 3-dihydroxy-6-nitro-7-sulfamoyl-benzo-(F)quinoxaline (NBQX), a competitive antagonist of the neuronal receptor for alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), or cis-4-[phosphono-methyl]-2-piperidine carboxylic acid (CGS 19755), a competitive antagonist of the N-methyl-d-aspartate (NMDA) receptor. After treatment, all animals were subjected to permanent occlusion of the middle cerebral artery for 6 or 24 h. Infarct volumes measured in animals pretreated with CGS 19755 after 24 h of ischemia were significantly smaller than those quantified in ischemic controls. Rats pretreated with NBQX showed partial amelioration of cytoskeletal injury with preserved immunolabeling of microtubule-associated protein 2 (MAP 2) at 6 and 24 h and reduced accumulation of calpain-cleaved spectrin byproducts only at 6 h. Prevention of cytoskeletal damage was more effective after pretreatment with CGS 19755, as shown by retention of MAP 2 immunolabeling and significant restriction of calpain activity at both 6 and 24 h.
2.L-glutamate excitation of A10 dopamine neurons is preferentially mediated by activation of NMDA receptors: extra- and intracellular electrophysiological studies in brain slices.
Wang T;French ED Brain Res. 1993 Nov 12;627(2):299-306.
The aim of the present study was to assess the effects of L-glutamate (L-GLU) on the neurophysiology of ventral tegmental A10 dopamine neurons in rat midbrain slices using extracellular and intracellular recording methods. L-Glutamate perfusion of 10-100 microM concentrations produced dose-dependent increases in firing rate, with no changes in pattern of firing, while higher concentrations led to a loss of activity reminiscent of depolarization inactivation. The extracellular changes were reflected by the pronounced membrane depolarizations observed through intracellular recordings. The effects of low doses (< or = 30 microM) of L-GLU on firing rate and membrane potential were completely antagonized by co-perfusion with the noncompetitive NMDA blocker, phencyclidine, or the selective competitive NMDA receptor antagonist, CGS 19755, but not by the selective non-NMDA blocker NBQX. However, at concentrations of > or = 300 microM L-GLU's effects could not be completely blocked without the presence of both CGS 19755 and NBQX. Moreover, the magnitude of L-GLU-induced depolarizations became attenuated at membrane potentials more negative than -70 mV. These results suggest that in physiological-like conditions that low extracellular levels of glutamate excite midbrain dopamine neurons via a preferential activation of NMDA receptors, and that only at higher concentrations of L-GLU are non-NMDA receptors brought into play.
3.SPD 502: a water-soluble and in vivo long-lasting AMPA antagonist with neuroprotective activity.
Nielsen EO;Varming T;Mathiesen C;Jensen LH;Moller A;Gouliaev AH;Wätjen F;Drejer J J Pharmacol Exp Ther. 1999 Jun;289(3):1492-501.
Accumulating preclinical data suggest that compounds that block the excitatory effect of glutamate on excitatory amino acid receptors may have neuroprotective effects and utility for the treatment of neurodegeneration after brain ischemia. In the present study, the in vitro and in vivo pharmacological properties of the novel glutamate antagonist SPD 502 [8-methyl-5(4-(N,N-dimethylsulfamoyl)phenyl)-6,7, 8,9,-tetrahydro-1H-pyrrolo[3,2-h]-isoquinoline-2, 3-dione-3-O-(4-hydroxybutyric acid-2-yl)oxime] are described. In binding studies, SPD 502 was shown to display selectivity for the [3H]alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-binding site (IC50 = 0.043 microM) compared with the [3H]kainate- (IC50 = 81 microM), [3H]cis-4-phosphonomethyl-2-piperidine carboxylic acid-(CGS 19755), and [3H]glycine-binding sites (IC50 > 30 microM) in rat cortical membranes. In an in vitro functional assay, SPD 502 blocked the AMPA-induced release of [3H]gamma-aminobutyric acid from cultured mouse cortical neurons in a competitive manner with an IC50 value of 0.23 microM. Furthermore, SPD 502 potently and selectively inhibited AMPA-induced currents in cortical neurons with an IC50 value of 0.
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CAS 110347-85-8 CGS 19755

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