Talampanel

Talampanel

Clinical data
ATC code	none
Legal status
Legal status	Investigational
Identifiers
IUPAC name (8R)-7-Acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h] [2,3]benzodiazepine
CAS Number	161832-65-1
PubChem (CID)	164509
ChemSpider	144217
UNII	CVS43XG1L5
ChEMBL	CHEMBL61872
ECHA InfoCard	100.230.001
Chemical and physical data
Formula	C19H19N3O3
Molar mass	337.372 g/mol
3D model (Jmol)	Interactive image
SMILES Nc4ccc(cc4)C(=NN2C(=O)C)c3cc1OCOc1cc3CC2C
InChI InChI=1S/C19H19N3O3/c1-11-7-14-8-17-18(25-10-24-17)9-16(14)19(21-22(11)12(2)23)13-3-5-15(20)6-4-13/h3-6,8-9,11H,7,10,20H2,1-2H3/t11-/m1/s1 Key:JACAAXNEHGBPOQ-LLVKDONJSA-N
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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]

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.