127910-32-1

127910-32-1 structure

Name: CGP 39551
Chemical Name: [(E)-4-amino-5-ethoxy-2-methyl-5-oxopent-2-enyl]phosphonic acid
CAS Number: 127910-32-1
Molecular Formula: C₈H₁₆NO₅P
Molecular Weight: 237.19
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2018-12-31 11:48:53
Modify Date: 2024-01-10 15:49:57
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity[1]. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM)[2].

Name	[(E)-4-amino-5-ethoxy-2-methyl-5-oxopent-2-enyl]phosphonic acid
Synonyms	2-Amino-4-methyl-5-phosphono-3 pentenoic acid carboxyethyl ester

Description	CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity[1]. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM)[2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> iGluR Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
In Vitro	CGP 39551 inhibits the binding of the selective NMDA receptor antagonist, [3H]-CPP to rat brain postsynaptic densities (PSDs) with a Ki of 310 nM[2].
In Vivo	CGP 39551 exhibits maximal electroshock-induced seizures in mice with the ED50 of 4 mg/kg (p.o.)[2]. Following chronic neonatal treatment with CGP 39551, adult rats show increased behavioral responses to the D2 dopamine receptor stimulation[3].
References	[1]. G E Fagg,et al. CGP 37849 and CGP 39551: novel competitive N-methyl-D-aspartate receptor antagonists with potent oral anticonvulsant activity. Prog Clin Biol Res. 1990;361:421-7. [2]. G E Fagg, 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. [3]. R Dall'Olio, et al. Chronic neonatal blockade of N-methyl-D-aspartate receptor by CGP 39551 increases dopaminergic function in adult rat. Neuroscience. 1994 Nov;63(2):451-5.