Talampanel

Talampanel, epilepsi^[1]^[2] malign gliomalar,^[3] ve amyotrofik lateral skleroz (ALS) tedavisi için araştırılmış bir ilaçtır.^[4]

Mayıs 2010 itibarıyla, ALS denemesinin sonuçları olumsuz bulunmuştur.^[5] Talampanel şu anda geliştirme aşamasında değildir.

Talampanel, merkezi sinir sisteminde bir tür iyonotropik glutamat reseptörü olan AMPA reseptörünün rekabetçi olmayan bir antagonisti olarak işlev görür.^[6]

Klinik çalışmalarda epilepsi için etkinlik göstermiştir ancak zayıf farmakokinetik profili, yani günde birden fazla doz gerektiren kısa bir terminal yarılanma ömrü (3 saat) nedeniyle gelişimi askıya alınmıştır.^[7]

Kaynakça

^ Luszczki (2009). "Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions". Pharmacological Reports. 61 (2): 197-216. doi:10.1016/s1734-1140(09)70024-6. PMID 19443931.
^ Bialer (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.
^ Iwamoto (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.
^ Pascuzzi (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.
^ Talampanel Trial 23 Mart 2011 tarihinde Wayback Machine sitesinde arşivlendi., Talampanel Trial on alsa.org
^ Aujla (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.
^ "AMPA Receptors as Therapeutic Targets for Neurological Disorders". Adv Protein Chem Struct Biol. Advances in Protein Chemistry and Structural Biology. 103: 203-61. 2016. doi:10.1016/bs.apcsb.2015.10.004. ISBN 9780128047941. PMID 26920691.

[1] Luszczki (2009). "Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions". Pharmacological Reports. 61 (2): 197-216. doi:10.1016/s1734-1140(09)70024-6. PMID 19443931.

[2] Bialer (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 (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 (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 23 Mart 2011 tarihinde Wayback Machine sitesinde arşivlendi., Talampanel Trial on alsa.org

[6] Aujla (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.

[pmid26920691-7] "AMPA Receptors as Therapeutic Targets for Neurological Disorders". Adv Protein Chem Struct Biol. Advances in Protein Chemistry and Structural Biology. 103: 203-61. 2016. doi:10.1016/bs.apcsb.2015.10.004. ISBN 9780128047941. PMID 26920691.

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g t d Benzodiazepinler
1,4-Benzodiazepinler	2-Oksokuazepam 3-Hidroksiphenazepam Bromazepam BMS-906024 Delorazepam Demoksepam Desmetilflunitrazepam Devazepide Diazepam Diklazepam Difludiazepam Doksefazepam Elfazepam Etil dirazepat Etil karfluzepat Etil loflazepat Fenazepam Flubromazepam Fletazepam Fludiazepam Flunitrazepam Flurazepam Flutemazepam Flutoprazepam Fosazepam Gidazepam Halazepam İklazepam İrazepin Kamazepam Karburazepam Kenazepin Ketazolam Klordiazepoksid Klonazepam Kloniprazepam Klorazepat Kuazepam Lorazepam Lormetazepam Lufuradom Medazepam Meklonazepam Menitrazepam Metaklazepam Motrazepam N-Desalkilflurazepam Nifoksipam Nimetazepam Nitemazepam Nitrazepam Nitrazepat Nordazepam Nortetrazepam Oksazepam Pinazepam Pivoksazepam Prazepam Proflazepam QH-II-66 Reclazepam RO4491533 Ro05-4082 Ro5-4864 Ro07-5220 Ro07-9749 Ro20-8065 Ro20-8552 SH-I-048A Sinazepam Sinolazepam Siprazepam Sulazepam Temazepam Tetrazepam Tifluadom Timelotem Tolufazepam Triflunordazepam Tuklazepam Uldazepam
1,5-Benzodiazepinler	Arfendazam CP-1414S Klobazam Lofendazam Triflubazam
2,3-Benzodiazepinler	Girisopam GYKI-52466 GYKI-52895 Nerisopam Talampanel Tofisopam
Triazolobenzodiazepinler	Adinazolam Alprazolam Balovaptan Bromazolam Estazolam Fenazolam Fluadinazolam Flualprazolam Flubromazolam Flunitrazolam Klonazolam Nitrazolam Pirazolam Rilmazolam Triazolam
Imidazobenzodiazepinler	Bretazenil EVT-201 FG-8205 Flumazenil GL-II-73 İmidazenil ¹²³I-İomazenil Klimazolam L-655,708 Loprazolam Midazolam PWZ-029 Remimazolam Ro15-4513 Ro48-6791 Ro48-8684 Ro4938581 Sarmazenil SH-053-R-CH3-2′F
Oksazolobenzodiazepinler	Flutazolam Haloksazolam Kloksazolam Meksazolam Oksazolam
Thienodiazepinler	Bentazepam Klotiazepam Ro09-9212
Thienotriazolodiazepinler	α-Hidroksietizolam Apafant Brotizolam Klotizolam Deskloroklotizolam Deskloroetizolam Etizolam Flubrotizolam Fluklotizolam Fluetizolam İsrapafant JQ1 Metizolam Siklotizolam
Thienobenzodiazepinler	Olanzapin Telenzepin
Pyridodiazepinler	Lopirazepam
Pyridotriazolodiazepinler	Zapizolam
Pyrazolodiazepinler	Razobazam Ripazepam Zolazepam Zomebazam Zometapin
Pyrrolodiazepinler	Premazepam
Tetrahidroisokuinobenzodiazepinler	Klazolam
Pirrolobenzodiazepinler	Antramisin
Benzodiazepin ön ilaçlar	Alprazolam triazolobenzofenon Avizafon Rilmazafon