Talampanel

Talampanel
Systematic (IUPAC) name
(8R)-7-Acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h] [2,3]benzodiazepine
Clinical data
  • N/A
  • investigational
Identifiers
161832-65-1 
None
PubChem CID 164509
ChemSpider 144217 
UNII CVS43XG1L5 Yes
ChEMBL CHEMBL61872 
Chemical data
Formula C19H19N3O3
337.372 g/mol
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Talampanel (INN) (code names GYKI 537773, LY300164) is a drug which has been investigated for the treatment of epilepsy,[1][2] malignant gliomas[3] and amyotrophic lateral sclerosis (ALS).[4]

As of May 2010, results from the trial for ALS have been found negative.[5] Talampanel is not currently under development.

Talampanel acts as a non-competitive antagonist of the AMPA receptor, a type of glutamate receptor in the central nervous system.[6]

See also

References

  1. ↑ Luszczki, J. J. (2009). "Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions". Pharmacological reports : PR 61 (2): 197–216. doi:10.1016/s1734-1140(09)70024-6. PMID 19443931.
  2. ↑ Bialer, M.; Johannessen, S. I.; Kupferberg, H. J.; Levy, R. H.; Perucca, E.; Tomson, T. R. (2007). "Progress report on new antiepileptic drugs: A summary of the Eighth Eilat Conference (EILAT VIII)". Epilepsy Research 73 (1): 1–52. doi:10.1016/j.eplepsyres.2006.10.008. PMID 17158031.
  3. ↑ Iwamoto, F. M.; Kreisl, T. N.; Kim, L.; Duic, J. P.; Butman, J. A.; Albert, P. S.; Fine, H. A. (2010). "Phase II Trial of Talampanel, a Glutamate Receptor Inhibitor, for Adults with Recurrent Malignant Gliomas". Cancer 116 (7): 1776–1782. doi:10.1002/cncr.24957. PMC 2846997. PMID 20143438.
  4. ↑ Pascuzzi, R. M.; Shefner, J.; Chappell, A. S.; Bjerke, J. S.; Tamura, R.; Chaudhry, V.; Clawson, L.; Haas, L.; Rothstein, J. D. (2009). "A phase II trial of talampanel in subjects with amyotrophic lateral sclerosis". Amyotrophic Lateral Sclerosis 11 (3): 266–271. doi:10.3109/17482960903307805. PMID 19961264.
  5. ↑ Talampanel Trial, Talampanel Trial on alsa.org
  6. ↑ Aujla, P. K.; Fetell, M. R.; Jensen, F. E. (2009). "Talampanel suppresses the acute and chronic effects of seizures in a rodent neonatal seizure model". Epilepsia 50 (4): 694–701. doi:10.1111/j.1528-1167.2008.01947.x. PMC 2672962. PMID 19220413.