CGP 37849

Names

[ Name ]:
CGP 37849

[Synonym ]:
Proglumide sodium salt
E-2-amino-4-methyl-5-phosphono-3-pentenoic acid
dl-2-amino-4-methyl-5-phosphono-3-*pentenoic acid

Biological Activity

[Description]:

CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[In Vitro]

In the hippocampal slice in vitro, CGP 37849 selectively and reversibly antagonizes NMDA-evoked increases in CA1 pyramidal cell firing rate. In slices bathed in medium containing low Mg2+ levels, concentrations of CGP 37849 up to 10 μM suppresses burst firing evoked in CA1 neurones by stimulation of Schaffer collateral-commissural fibres without affecting the magnitude of the initial population spike[1].

[In Vivo]

CGP 37849 potently (Ki of 220 nM) and competitively inhibits NMDA-sensitive l-[3H]-glutamate binding to postsynaptic density (PSD) fractins from rat brain. CGP 37849 inhibits the binding of the selective NMDA receptor antagonist, [3H]-(±)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonate (CPP), with a Ki of 35 nM[1]. In vivo, oral administration to rats of CGP 37849 selectively blocks firing in hippocampal neurones induced by ionophoretically-applied NMDA, without affecting the responses to quisqualate or kainate[1]. Oral administration to mice of CGP 37849 suppresses maximal electroshock-induced seizures in mice with an ED50 of 21 mg/kg[1].

[References]

[1]. Fagg GE, et al. CGP 37849 and CGP 39551: novel and potent competitive N-methyl-D-aspartate receptor antagonists with oral activity. Br J Pharmacol. 1990 Apr;99(4):791-7.

[2]. Schmutz M, et al. The competitive NMDA receptor antagonists CGP 37849 and CGP 39551 are potent, orally-active anticonvulsants in rodents. Naunyn Schmiedebergs Arch Pharmacol. 1990 Jul;342(1):61-6.

[3]. Papp M, et al. Antidepressant activity of non-competitive and competitive NMDA receptor antagonists in a chronic mild stress model of depression. Eur J Pharmacol. 1994 Sep 22;263(1-2):1-7.

[4]. Przegaliński E, et al. The influence of the benzodiazepine receptor antagonist flumazenil on the anxiolytic-like effects of CGP 37849 and ACPC in rats. Neuropharmacology. 2000 Jul 24;39(10):1858-64.

Chemical & Physical Properties

[ Density]:
1.506 g/cm3

[ Boiling Point ]:
523.1ºC at 760 mmHg

[ Molecular Formula ]:
C₆H₁₂NO₅P

[ Molecular Weight ]:
209.13700

[ Flash Point ]:
270.2ºC

[ Exact Mass ]:
209.04500

[ PSA ]:
130.66000

[ LogP ]:
0.22260

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Precursor & DownStream

Precursor

DownStream

Articles

Involvement of voltage- and ligand-gated Ca2+ channels in the neuroexcitatory and synergistic effects of putative uremic neurotoxins.

Kidney Int. 63(5) , 1764-75, (2003)

Renal failure has been viewed as a state of cellular calcium toxicity due to the retention of small fast-acting molecules. We have tested this hypothesis and identified potentially neuroexcitatory com...

GSA: behavioral, histological, electrophysiological and neurochemical effects.

Physiol. Behav. 84(2) , 251-64, (2005)

Renal insufficient patients suffer from a variety of complications as direct and indirect consequence of accumulation of retention solutes. Guanidinosuccinic acid (GSA) is an important probable uremic...

Competitive NMDA receptor antagonists and agonists: effects on spontaneous alternation in mice exposed to cerebral oligemia.

Pol. J. Pharmacol. 56(1) , 59-66, (2004)

The purpose of the present study was to investigate the effects of competitive NMDA receptor antagonists,D,L-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid (CGP 37849) and its ethyl ester (CGP 3955...