CGP-37849

CGP-37849 is a competitive antagonist at the NMDA receptor.[1] It is a potent, orally active anticonvulsant in animal models,[2] and was researched for the treatment of epilepsy.[3] It also has neuroprotective activity[4] and shows antidepressant[5][6] and anxiolytic effects.[7][8]

CGP-37849
Clinical data
Other namesCGP-37849, CGP-40116
Identifiers
IUPAC name
  • (E,2R)-2-amino-4-methyl-5-phosphonopent-3-enoic acid
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC6H12NO5P
Molar mass209.138 g·mol−1
3D model (JSmol)
SMILES
  • C/C(=C\[C@H](C(=O)O)N)/CP(=O)(O)O
InChI
  • InChI=1S/C6H12NO5P/c1-4(3-13(10,11)12)2-5(7)6(8)9/h2,5H,3,7H2,1H3,(H,8,9)(H2,10,11,12)/b4-2+/t5-/m1/s1 N
  • Key:BDYHNCZIGYIOGJ-XWCPEMDWSA-N N
 NY (what is this?)  (verify)

References
  1. Fagg GE, Olpe HR, Pozza MF, Baud J, Steinmann M, Schmutz M, et al. (April 1990). "CGP 37849 and CGP 39551: novel and potent competitive N-methyl-D-aspartate receptor antagonists with oral activity". British Journal of Pharmacology. 99 (4): 791–7. doi:10.1111/j.1476-5381.1990.tb13008.x. PMC 1917531. PMID 1972895.
  2. Schmutz M, Portet C, Jeker A, Klebs K, Vassout A, Allgeier H, et al. (July 1990). "The competitive NMDA receptor antagonists CGP 37849 and CGP 39551 are potent, orally-active anticonvulsants in rodents". Naunyn-Schmiedeberg's Archives of Pharmacology. 342 (1): 61–6. doi:10.1007/bf00178973. PMID 1976233. S2CID 25531153.
  3. Fujikawa DG, Daniels AH, Kim JS (March 1994). "The competitive NMDA receptor antagonist CGP 40116 protects against status epilepticus-induced neuronal damage". Epilepsy Research. 17 (3): 207–19. doi:10.1016/0920-1211(94)90051-5. PMID 7912191. S2CID 13656613.
  4. Gutnikov SA, Gaffan D (June 1996). "Systemic NMDA receptor antagonist CGP-40116 does not impair memory acquisition but protects against NMDA neurotoxicity in rhesus monkeys". The Journal of Neuroscience. 16 (12): 4041–5. doi:10.1523/JNEUROSCI.16-12-04041.1996. PMC 6578604. PMID 8656297.
  5. Maj J, Klimek V, Gołembiowska K, Rogóz Z, Skuza G (1993). "Central effects of repeated treatment with CGP 37849, a competitive NMDA receptor antagonist with potential antidepressant activity". Polish Journal of Pharmacology. 45 (5–6): 455–66. PMID 7912134.
  6. Papp M, Moryl E (September 1994). "Antidepressant activity of non-competitive and competitive NMDA receptor antagonists in a chronic mild stress model of depression". European Journal of Pharmacology. 263 (1–2): 1–7. doi:10.1016/0014-2999(94)90516-9. PMID 7821340.
  7. Jessa M, Nazar M, Bidzinski A, Plaznik A (March 1996). "The effects of repeated administration of diazepam, MK-801 and CGP 37849 on rat behavior in two models of anxiety". European Neuropsychopharmacology. 6 (1): 55–61. doi:10.1016/0924-977x(95)00068-z. PMID 8866939. S2CID 45953054.
  8. Przegaliński E, Tatarczyńska E, Chojnacka-Wójcik E (July 2000). "The influence of the benzodiazepine receptor antagonist flumazenil on the anxiolytic-like effects of CGP 37849 and ACPC in rats". Neuropharmacology. 39 (10): 1858–64. doi:10.1016/s0028-3908(00)00023-x. PMID 10884566. S2CID 33660694.
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