他侖帕奈

他侖帕奈
臨床資料
ATC碼	未分配;
法律規範狀態
法律規範	研究性藥物;
識別資訊
	IUPAC命名法 (8R)-7-Acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine; ;
CAS號	161832-65-1
PubChem CID	164509;
ChemSpider	144217 ;
UNII	CVS43XG1L5;
ChEMBL	ChEMBL61872 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID10167259 ;
ECHA InfoCard	100.230.001
化學資訊
化學式	C19H19N3O3
摩爾質量	337.38 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	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 ;

他侖帕奈（INN：Talampanel；研發代號：GYKI 537773和LY300164）是一種已被研究用於治療癲癇、^[1]^[2]惡性神經膠質瘤^[3]和肌萎縮側索硬化的藥物。^[4]

截至2010年5月，對於肌萎縮側索硬化的試驗結果呈負面的。^[5]他侖帕奈目前已經不再開發。

他侖帕奈作為AMPA受體的非競爭性拮抗劑，AMPA受體是中樞神經系統中的一種離子型穀氨酸受體。

它在臨床試驗中顯示出對癲癇有效，但由於其藥代動力學特徵不佳，即終末半衰期短（3小時），需要每天多次給藥，因此其開發被暫停。^[6]

參考資料

^ Luszczki, J. J. Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions. Pharmacological Reports. 2009, 61 (2): 197–216. PMID 19443931. doi:10.1016/s1734-1140(09)70024-6.
^ Bialer, M.; Johannessen, S. I.; Kupferberg, H. J.; Levy, R. H.; Perucca, E.; Tomson, T. R. Progress report on new antiepileptic drugs: A summary of the Eighth Eilat Conference (EILAT VIII). Epilepsy Research. 2007, 73 (1): 1–52. PMID 17158031. S2CID 45026113. doi:10.1016/j.eplepsyres.2006.10.008.
^ Iwamoto, F. M.; Kreisl, T. N.; Kim, L.; Duic, J. P.; Butman, J. A.; Albert, P. S.; Fine, H. A. Phase II Trial of Talampanel, a Glutamate Receptor Inhibitor, for Adults with Recurrent Malignant Gliomas. Cancer. 2010, 116 (7): 1776–1782. PMC 2846997  . PMID 20143438. doi:10.1002/cncr.24957.
^ Pascuzzi, R. M.; Shefner, J.; Chappell, A. S.; Bjerke, J. S.; Tamura, R.; Chaudhry, V.; Clawson, L.; Haas, L.; Rothstein, J. D. A phase II trial of talampanel in subjects with amyotrophic lateral sclerosis. Amyotrophic Lateral Sclerosis. 2009, 11 (3): 266–271. PMID 19961264. S2CID 7388452. doi:10.3109/17482960903307805.
^ Talampanel Trial （頁面存檔備份，存於互聯網檔案館）, Talampanel Trial on alsa.org
^ Lee K, Goodman L, Fourie C, Schenk S, Leitch B, Montgomery JM. AMPA Receptors as Therapeutic Targets for Neurological Disorders. Adv Protein Chem Struct Biol. Advances in Protein Chemistry and Structural Biology. 2016, 103: 203–61. ISBN 9780128047941. PMID 26920691. doi:10.1016/bs.apcsb.2015.10.004.

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

[2] Bialer, M.; Johannessen, S. I.; Kupferberg, H. J.; Levy, R. H.; Perucca, E.; Tomson, T. R. Progress report on new antiepileptic drugs: A summary of the Eighth Eilat Conference (EILAT VIII). Epilepsy Research. 2007, 73 (1): 1–52. PMID 17158031. S2CID 45026113. doi:10.1016/j.eplepsyres.2006.10.008.

[3] Iwamoto, F. M.; Kreisl, T. N.; Kim, L.; Duic, J. P.; Butman, J. A.; Albert, P. S.; Fine, H. A. Phase II Trial of Talampanel, a Glutamate Receptor Inhibitor, for Adults with Recurrent Malignant Gliomas. Cancer. 2010, 116 (7): 1776–1782. PMC 2846997  . PMID 20143438. doi:10.1002/cncr.24957.

[4] Pascuzzi, R. M.; Shefner, J.; Chappell, A. S.; Bjerke, J. S.; Tamura, R.; Chaudhry, V.; Clawson, L.; Haas, L.; Rothstein, J. D. A phase II trial of talampanel in subjects with amyotrophic lateral sclerosis. Amyotrophic Lateral Sclerosis. 2009, 11 (3): 266–271. PMID 19961264. S2CID 7388452. doi:10.3109/17482960903307805.

[5] Talampanel Trial （頁面存檔備份，存於互聯網檔案館）, Talampanel Trial on alsa.org

[pmid26920691-6] Lee K, Goodman L, Fourie C, Schenk S, Leitch B, Montgomery JM. AMPA Receptors as Therapeutic Targets for Neurological Disorders. Adv Protein Chem Struct Biol. Advances in Protein Chemistry and Structural Biology. 2016, 103: 203–61. ISBN 9780128047941. PMID 26920691. doi:10.1016/bs.apcsb.2015.10.004.

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臨床資料

ATC碼	未分配
法律規範狀態
法律規範	研究性藥物
識別資訊
IUPAC命名法 (8R)-7-Acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine
CAS號	161832-65-1 ^Y
PubChem CID	164509
ChemSpider	144217^N
UNII	CVS43XG1L5
ChEMBL	ChEMBL61872^N
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID10167259
ECHA InfoCard	100.230.001
化學資訊
化學式	C₁₉H₁₉N₃O₃
摩爾質量	337.38 g·mol⁻¹
3D模型（JSmol（英語：JSmol））	交互式圖像
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^N Key:JACAAXNEHGBPOQ-LLVKDONJSA-N^N