2-amino-4-methyl-5-phosphono-3-pentenoic acid

N-methyl-D-aspartate receptor antagonist; structure given in first source; RN given refers to cpd without isomeric designation; CGP-40116 is the (R)-enantiomer of CGP-37849; CGP-40017 is the L-isomer

Also Known As:

2-amino-4-methyl-5-phosphono-3-pentenoic acid, (E)-isomer; 2-amino-4-methyl-5-phosphono-3-pentenoic acid, E(+-)-isomer; 2-amino-4-methyl-5-phosphono-3-pentenoic acid, R-(E)-isomer; 2-amino-4-methyl-5-phosphono-3-pentenoic acid, S-(E)-isomer; 4-methyl-APPA; CGP 37849; CGP 40017; CGP 40116; CGP-37849; CGP-40017; CGP-40116; CGP40.116; 3-Pentenoic acid, 2-amino-4-methyl-5-phosphono-, (E)-(+-)-

Networked: 49 relevant articles (1 outcomes, 2 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Amino Acids, Peptides, and Proteins: 1
- Amino Acids: 30675
  - Branched-Chain Amino Acids: 2289
    - Valine: 1999
      - 2-Amino-5-phosphonovalerate: 94
        2-amino-4-methyl-5-phosphono-3-pentenoic acid: 49
  - Phosphoamino Acids: 1
    - 2-Amino-5-phosphonovalerate: 94
      - 2-amino-4-methyl-5-phosphono-3-pentenoic acid: 49

Experts

1.	Czuczwar, S J: 2 articles (10/2000 - 01/2000)
2.	Kleinrok, Z: 2 articles (10/2000 - 01/2000)
3.	Rejdak, K: 2 articles (10/2000 - 01/2000)
4.	Rejdak, R: 2 articles (10/2000 - 01/2000)
5.	Sieklucka-Dziuba, M: 2 articles (10/2000 - 01/2000)
6.	Nieoczym, Dorota: 1 article (11/2018)
7.	Socała, Katarzyna: 1 article (11/2018)
8.	Wlaź, Piotr: 1 article (11/2018)
9.	Mares, Pavel: 1 article (05/2005)
10.	Slamberová, Romana: 1 article (05/2005)

Related Diseases

1.	Status Epilepticus (Complex Partial Status Epilepticus) 03/01/1994 - "The competitive NMDA receptor antagonist CGP 40116 protects against status epilepticus-induced neuronal damage." 03/01/1994 - "We studied the efficacy of the competitive NMDA receptor antagonist CGP 40116 in protecting against seizure-induced neuronal necrosis from lithium-pilocarpine-induced status epilepticus (SE). "
2.	Necrosis 03/01/1994 - "No necrotic neurons were found in posterior cingulate and retrosplenial neurons at the two highest CGP 40116 doses, suggesting that the transient cytoplasmic vacuolization induced by NMDA receptor antagonists does not progress to frank necrosis. " 03/01/1994 - "CGP 40116 provided widespread protection against seizure-induced neuronal necrosis, suggesting that an essential step in its production is NMDA receptor activation by endogenous glutamate. " 03/01/1994 - "We studied the efficacy of the competitive NMDA receptor antagonist CGP 40116 in protecting against seizure-induced neuronal necrosis from lithium-pilocarpine-induced status epilepticus (SE). "
3.	Brain Ischemia (Cerebral Ischemia) 10/01/2000 - "The effect of CGP-40116 on pilocarpine evoked seizures in mice exposed to transient episode of brain ischemia." 07/01/1995 - "Our results indicate that (a) the competitive NMDA antagonist CGP 40116 permanently protects brain tissue from the consequences of cerebral ischemia in a rat model for human stroke and (b) early and late pathological changes can be accurately measured by MRI." 07/01/1995 - "In this study we evaluated the effect of the competitive N-methyl-D-aspartate (NMDA) antagonist D-(E)-4-(3-phosphonoprop-2-enyl)piperazine-2-carboxylic acid (CGP 40116) on both early (2 days) and late (28 days) ischemic brain damage in a rodent model of focal cerebral ischemia by means of magnetic resonance imaging (MRI) and conventional histology. " 06/01/1997 - "Effect of the new competitive N-methyl-D-aspartate (NMDA) antagonist D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid (CAS 137424-81-8, CGP 40116) was examined in a mongolian gerbil model of global cerebral ischemia. " 06/01/1997 - "The effect of the new competitive N-methyl-D-aspartate (NMDA) antagonist D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid (CAS 137424-81-8, CGP 40116) was examined in a cat model of focal cerebral ischemia. "
4.	Anxiety Disorders (Anxiety Disorder) 05/01/1996 - "These results, as well as the literature data on the lack of motor-impairing effects of ACPC, indicate that the latter drug seems to be more advantageous than CGP 37849 as a potential therapeutic agent in the treatment of anxiety disorders. " 03/01/1996 - "It is concluded that the new class of competitive NMDA receptor antagonists, exemplified by CGP 37849, is the most promising candidate for clinical trials in anxiety disorders."
5.	Seizures (Absence Seizure) 01/01/1998 - "Pretreatment with CGP 40116 did not influence minimal, predominantly clonic seizures in any age group. " 09/23/1996 - "Following 2 and 4 weeks of repeated drug administration with CGP 37849 (20 and 40 mumol kg-1) the ED50 values against clonic and tonic seizures were not significantly different from those observed following an acute administration. " 09/23/1996 - "Acute administration of CGP 37849 attenuated the clonic and tonic phases of the audiogenic seizures (109 dB, 12-16 kHz) 120 min after pretreatment (ED50 19.7 and 11.2 mumol kg-1, respectively). " 07/01/1990 - "At optimal pretreatment times CGP 37849 suppressed electroshock-induced seizures in mice and rats with ED50s ranging from 8 to 22 mg/kg after oral administration, and 0.4 to 2.4 mg/kg after i.v. and i.p. " 05/23/2005 - "Duration of afterdischarges was reduced and intensity of clonic seizures was decreased by CGP 40116 in all age groups; dizocilpine exhibited similar action in 25- and 18-day-old rats, AP7 only in 25-day-old animals. "

Related Drugs and Biologics

1.	N-Methyl-D-Aspartate Receptors (NMDA Receptors)
2.	Pilocarpine (Ocusert)
3.	Glutamic Acid (Glutamate)
4.	Lithium
5.	N-Methylaspartate (NMDA)
6.	Acids
7.	Dizocilpine Maleate (Dizocilpine)
8.	CGP 39551
9.	Anticonvulsants (Antiepileptic Drugs)
10.	Memantine (Namenda)

Related Therapies and Procedures

1.	Oral Administration
2.	Therapeutics