Talampanel

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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
Pregnancy cat.	?
Legal status	investigational
Identifiers
CAS number	161832-65-1^N
ATC code	None
PubChem	CID 164509
UNII	CVS43XG1L5^Y
ChEMBL	CHEMBL61872^N
Chemical data
Formula	C₁₉H₁₉N₃O₃
Mol. mass	337.372 g/mol
SMILES	eMolecules & PubChem
N (what is this?) (verify)

Talampanel (GYKI 53405) is a drug which is being investigated for the treatment of epilepsy,^[1] malignant gliomas^[2] and amyotrophic lateral sclerosis (ALS).^[3].

As of May 2010, results from the trial for ALS have been found negative.^[4]

It is a noncompetitive antagonist of the AMPA receptor, a type of glutamate receptor in the central nervous system.^[5]

[edit] References

^ Luszczki, J. J. (2009). "Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions". Pharmacological reports : PR 61 (2): 197–216. PMID 19443931. edit
^ 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. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2846997. edit
^ Pascuzzi, R. M.; Shefner, J.; Chappell, A. S.; Bjerke, J. S.; Tamura, R.; Chaudhry, V.; Clawson, L.; Haas, L. et al. (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. edit
^ Talampanel Trial, Talampanel Trial on alsa.org
^ 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. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2672962. edit

Glutamatergics

Ionotropic

AMPA	Agonists: 5-Fluorowillardiine AMPA Domoic acid Quisqualic acid; Positive allosteric modulators: Aniracetam Cyclothiazide CX-516 CX-546 CX-614 CX-691 CX-717 Diazoxide HCTZ IDRA-21 LY-392,098 LY-404,187 LY-451,395 LY-451,646 LY-503,430 Org 26576 Oxiracetam PEPA Piracetam Pramiracetam S-18986 Sunifiram Unifiram Antagonists: ATPO Barbiturates BGG492 Caroverine CNQX DNQX GYKI-52466 NBQX Perampanel Talampanel Tezampanel Topiramate; Negative allosteric modulators: GYKI-53,655

NMDA	Agonists: Glutamate/acite site competitive agonists: Aspartate Glutamate Homoquinolinic acid Ibotenic acid NMDA Quinolinic acid Tetrazolylglycine; Glycine site agonists: ACBD ACPC ACPD Alanine CCG Cycloserine DHPG Fluoroalanine Glycine HA-966 L-687,414 Milacemide Sarcosine Serine Tetrazolylglycine; Polyamine site agonists: Acamprosate Spermidine Spermine Antagonists: Competitive antagonists: AP5 (APV) AP7 CGP-37849 CGP-39551 CGP-39653 CGP-40116 CGS-19755 CPP LY-233,053 LY-235,959 LY-274,614 MDL-100,453 Midafotel (d-CPPene) NPC-12,626 NPC-17,742 PBPD PEAQX Perzinfotel PPDA SDZ-220581 Selfotel; Noncompetitive antagonists: ARR-15,896 Caroverine Dexanabinol FPL-12495 FR-115,427 Hodgkinsine Magnesium MDL-27,266 NPS-1506 Psychotridine Zinc; Uncompetitive pore blockers: 2-MDP 3-MeO-PCP 8A-PDHQ Alaproclate Amantadine Aptiganel ARL-12,495 ARL-15,896-AR ARL-16,247 Budipine Delucemine Dexoxadrol Dextrallorphan Dieticyclidine Dizocilpine Endopsychosin Esketamine Etoxadrol Eticyclidine Gacyclidine Ibogaine Indantadol Ketamine Ketobemidone Loperamide Memantine Meperidine (Pethidine) Methadone (Levomethadone) Methorphan (Dextromethorphan Levomethorphan) Methoxetamine Milnacipran Morphanol (Dextrorphan Levorphanol) NEFA Neramexane Nitrous oxide Noribogaine Orphenadrine PCPr Phencyclamine Phencyclidine Propoxyphene Remacemide Rhynchophylline Riluzole Rimantadine Rolicyclidine Sabeluzole Tenocyclidine Tiletamine Tramadol Xenon; Glycine site antagonists: ACEA-1021 ACEA-1328 ACPC Carisoprodol CGP-39653 CKA DCKA Felbamate Gavestinel GV-196,771 Kynurenic acid L-689,560 L-701,324 Lacosamide Licostinel LU-73,068 MDL-105,519 Meprobamate MRZ 2/576 PNQX ZD-9379; NR2B subunit antagonists: Besonprodil CO-101,244 (PD-174,494) CP-101,606 Eliprodil Haloperidol Ifenprodil Isoxsuprine Nylidrin Ro8-4304 Ro25-6981 Traxoprodil; Polyamine site antagonists: Arcaine Co 101676 Diaminopropane Acamprosate Diethylenetriamine Huperzine A Putrescine Ro 25-6981; Unclassified/unsorted antagonists: Chloroform Diethyl ether Enflurane Ethanol (Alcohol) Halothane Isoflurane Methoxyflurane Toluene Trichloroethane Trichloroethanol Trichloroethylene Xylene

Kainate	Agonists: 5-Iodowillardiine ATPA Domoic acid Kainic acid LY-339,434 SYM-2081 Antagonists: BGG492 CNQX DNQX LY-382,884 NBQX NS102 Tezampanel Topiramate UBP-302; Negative allosteric modulators: NS-3763

Metabotropic

Group I	Agonists: Non-selective: ACPD DHPG Quisqualic acid; mGlu1-selective: Ro01-6128 Ro67-4853 Ro67-7476 VU-71; mGlu5-selective: ADX-47273 CDPPB CHPG DFB VU-1545 Antagonists: Non-selective: MCPG NPS-2390; mGlu1-selective: BAY 36-7620 CPCCOEt LY-367,385 LY-456,236; mGlu5-selective: CTEP Dipraglurant DMeOB LY-344,545 SIB-1757 SIB-1893; Negative allosteric modulators: Fenobam MPEP MTEP GRN-529

Group II	Agonists: Non-selective: CBiPES DCG-IV Eglumegad LY-379,268 LY-404,039 LY-487,379 MGS-0028; mGlu2-selective: BINA LY-566,332 Antagonists: Non-selective: APICA EGLU HYDIA LY-307,452 LY-341,495 MCPG MGS-0039: mGlu2-selective: PCCG-4; mGlu3-selective: CECXG; Negative allosteric modulators: RO4491533

Group III	Agonists: Non-selective: L-AP4; mGlu4-selective: PHCCC VU-001,171 VU-0155,041; mGlu7-selective: AMN082; mGlu8-selective: DCPG Antagonists: Non-selective: CPPG MAP4 MSOP MPPG MTPG UBP-1112; mGlu7-selective: MMPIP

Transporter
inhibitors

EAATs	DHKA PDC WAY-213,613

vGluTs	7-CKA Evans blue

Others

Precursors	L-Glutamine

Cofactors	α-Ketoglutaric acid Iron Sulfur Vitamin B2 (as FAD and FMN) Vitamin B3 (as NADPH)

Others	L-Theanine

v t e Benzodiazepine derivatives

1,4-Benzodiazepines	Bromazepam Camazepam Carburazepam Chlordiazepoxide Cinolazepam Clonazepam Clorazepate Cyprazepam Delorazepam Demoxepam Devazepide * Diazepam Doxefazepam Elfazepam Ethyl carfluzepate Ethyl dirazepate Ethyl loflazepate Fletazepam Fludiazepam Flunitrazepam Flurazepam Flutemazepam Flutoprazepam Fosazepam Gidazepam Halazepam Iclazepam Ketazolam Lorazepam Lormetazepam Lufuradom * Meclonazepam Medazepam Menitrazepam Metaclazepam Motrazepam Nimetazepam Nitrazepam Nitrazepate Nordazepam Nortetrazepam Oxazepam Phenazepam Pinazepam Pivoxazepam Prazepam Proflazepam Quazepam QH-II-66 Reclazepam RO4491533 * Ro5-2904 Ro5-4864 * Sulazepam Temazepam Tetrazepam Tifluadom * Tolufazepam Tuclazepam Uldazepam

1,5-Benzodiazepines	Arfendazam Clobazam CP-1414S Lofendazam Triflubazam

2,3-Benzodiazepines *	Girisopam GYKI-52466 GYKI-52895 Nerisopam Talampanel Tofisopam

Triazolobenzodiazepines	Adinazolam Alprazolam Estazolam Flubromazolam Triazolam

Imidazobenzodiazepines	Bretazenil Climazolam FG-8205 Flumazenil Imidazenil Iomazenil (¹²³I) L-655,708 Loprazolam Midazolam PWZ-029 Remimazolam Ro15-4513 Ro48-6791 Ro48-8684 Sarmazenil SH-053-R-CH3-2′F

Oxazolobenzodiazepines	Cloxazolam Flutazolam Haloxazolam Mexazolam Oxazolam

Thienodiazepines	Bentazepam Brotizolam Ciclotizolam Clotiazepam Etizolam Olanzapine *

Pyridodiazepines	Lopirazepam Zapizolam

Pyrazolodiazepines	Razobazam * Ripazepam Zolazepam Zomebazam

Pyrrolodiazepines	Premazepam

Tetrahydroisoquinobenzodiazepines	Clazolam

Benzodiazepine prodrugs	Avizafone Rilmazafone

* atypical activity profile (not GABA_A receptor ligands)

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