Chemistry:Talampanel
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Short description: Chemical compound
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| Formula | C19H19N3O3 |
| Molar mass | 337.379 g·mol−1 |
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Talampanel (INN; development codes GYKI 537773 and 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 ionotropic glutamate receptor in the central nervous system.[6]
It showed effectiveness for epilepsy in clinical trials but its development was suspended due to its poor pharmacokinetic profile, namely a short terminal half-life (3 hours) that necessitated multiple doses per day.[7]
References
- ↑ "Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions". Pharmacological Reports 61 (2): 197–216. 2009. doi:10.1016/s1734-1140(09)70024-6. PMID 19443931.
- ↑ "Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII)". Epilepsy Research 73 (1): 1–52. January 2007. doi:10.1016/j.eplepsyres.2006.10.008. PMID 17158031.
- ↑ "Phase 2 trial of talampanel, a glutamate receptor inhibitor, for adults with recurrent malignant gliomas". Cancer 116 (7): 1776–1782. April 2010. doi:10.1002/cncr.24957. PMID 20143438.
- ↑ "A phase II trial of talampanel in subjects with amyotrophic lateral sclerosis". Amyotrophic Lateral Sclerosis 11 (3): 266–271. May 2010. doi:10.3109/17482960903307805. PMID 19961264.
- ↑ "Talampanel Trial". alsa.org. May 2010. http://www.alsa.org/research/clinical-trials/talampanel-trial.html.
- ↑ "Talampanel suppresses the acute and chronic effects of seizures in a rodent neonatal seizure model". Epilepsia 50 (4): 694–701. April 2009. doi:10.1111/j.1528-1167.2008.01947.x. PMID 19220413.
- ↑ AMPA Receptors as Therapeutic Targets for Neurological Disorders. Advances in Protein Chemistry and Structural Biology. 103. 2016. pp. 203–261. doi:10.1016/bs.apcsb.2015.10.004. ISBN 9780128047941. PMID 26920691.
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