他仑帕奈

他仑帕奈
臨床資料
ATC碼	未分配;
法律規範狀態
法律規範	研究性药物;
识别信息
	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号	161832-65-1
PubChem CID	164509;
ChemSpider	144217 ;
UNII	CVS43XG1L5;
ChEMBL	ChEMBL61872 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID10167259 ;
ECHA InfoCard	100.230.001
化学信息
化学式	C19H19N3O3
摩尔质量	337.38 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	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 ;

他仑帕奈（INN：Talampanel；研发代号：GYKI 537773和LY300164）是一种已被研究用于治疗癫痫、^[1]^[2]恶性神经胶质瘤^[3]和肌萎缩侧索硬化的药物。^[4]

截至2010年5月，对于肌萎缩侧索硬化的试验结果呈负面的。^[5]他仑帕奈目前已经不再开发。

他仑帕奈作为AMPA受体的非竞争性拮抗剂，AMPA受体是中枢神经系统中的一种离子型谷氨酸受体。

它在临床试验中显示出对癫痫有效，但由于其药代动力学特征不佳，即终末半衰期短（3小时），需要每天多次给药，因此其开发被暂停。^[6]

参考资料

^ 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 （页面存档备份，存于互联网档案馆）, 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 （页面存档备份，存于互联网档案馆）, 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	研究性药物
识别信息
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号	161832-65-1 ^Y
PubChem CID	164509
ChemSpider	144217^N
UNII	CVS43XG1L5
ChEMBL	ChEMBL61872^N
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID10167259
ECHA InfoCard	100.230.001
化学信息
化学式	C₁₉H₁₉N₃O₃
摩尔质量	337.38 g·mol⁻¹
3D模型（JSmol（英语：JSmol））	交互式图像
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