Tiagabine (BioDeep_00000002678)

 

Secondary id: BioDeep_00000406040

human metabolite blood metabolite


代谢物信息卡片


(R)-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)-3-piperidinecarboxylic acid, hydrochloride

化学式: C20H25NO2S2 (375.132663)
中文名称: 盐酸替加滨
谱图信息: 最多检出来源 Homo sapiens(blood) 0.71%

分子结构信息

SMILES: CC1=C(SC=C1)C(=CCCN1CCC[C@H](C1)C(O)=O)C1=C(C)C=CS1
InChI: InChI=1S/C20H25NO2S2/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23)/t16-/m1/s1

描述信息

Tiagabine is an anti-convulsive medication. It is also used in the treatment for panic disorder as are a few other anticonvulsants. Though the exact mechanism by which tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor.
D018377 - Neurotransmitter Agents > D014179 - Neurotransmitter Uptake Inhibitors > D058805 - GABA Uptake Inhibitors
N - Nervous system > N03 - Antiepileptics > N03A - Antiepileptics > N03AG - Fatty acid derivatives
C78272 - Agent Affecting Nervous System > C264 - Anticonvulsant Agent
D002491 - Central Nervous System Agents > D000927 - Anticonvulsants
D018377 - Neurotransmitter Agents > D018682 - GABA Agents
D049990 - Membrane Transport Modulators

同义名列表

17 个代谢物同义名

(R)-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)-3-piperidinecarboxylic acid, hydrochloride; (3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidine-3-carboxylic acid; (-)-(R)-1-[4,4-Bis(3-methyl-2-thienyl)-3butenyl]nipecotic acid hydrochloride; (R)-(-)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid; (-)-(R)-1-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)nipecotic acid; (-)-(R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid; (-)-(R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotate; (R)-(-)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotate; (-)-(R)-1-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)nipecotate; N-(4,4-Di(3-methylthien-2-yl)but-3-enyl)nipecotic acid; Tiagabine hydrochloride; Tiagabine, (S)-isomer; (R)-Tiagabine; Tiagabinum; Tiagabina; Tiagabine; Gabitril



数据库引用编号

19 个数据库交叉引用编号

分类词条

相关代谢途径

Reactome(0)

BioCyc(0)

PlantCyc(0)

代谢反应

0 个相关的代谢反应过程信息。

Reactome(0)

BioCyc(0)

WikiPathways(0)

Plant Reactome(0)

INOH(0)

PlantCyc(0)

COVID-19 Disease Map(0)

PathBank(0)

PharmGKB(0)

1 个相关的物种来源信息

在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：

  • PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
  • NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
  • Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
  • Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。



文献列表

  • Sana Javaid, Faleh Alqahtani, Waseem Ashraf, Syed Muhammad Muneeb Anjum, Muhammad Fawad Rasool, Tanveer Ahmad, Fawaz Alasmari, Abdullah F Alasmari, Saleh Abdullah Alqarni, Imran Imran. Tiagabine suppresses pentylenetetrazole-induced seizures in mice and improves behavioral and cognitive parameters by modulating BDNF/TrkB expression and neuroinflammatory markers. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2023 Feb; 160(?):114406. doi: 10.1016/j.biopha.2023.114406. [PMID: 36791567]
  • Zenia Motiwala, Nanda Gowtham Aduri, Hamidreza Shaye, Gye Won Han, Jordy Homing Lam, Vsevolod Katritch, Vadim Cherezov, Cornelius Gati. Structural basis of GABA reuptake inhibition. Nature. 2022 06; 606(7915):820-826. doi: 10.1038/s41586-022-04814-x. [PMID: 35676483]
  • Sadia Zafar, Ishrat Jabeen. Molecular Dynamic Simulations to Probe Stereoselectivity of Tiagabine Binding with Human GAT1. Molecules (Basel, Switzerland). 2020 Oct; 25(20):. doi: 10.3390/molecules25204745. [PMID: 33081136]
  • Zhen Zou, Xiaodou Liao, Le Yang, Ziyun Huang, Hua Yang, Qi Yan, Yufei Zhang, Zhihe Qing, Lihua Zhang, Feng Feng, Ronghua Yang. Human Serum Albumin-Occupying-Based Fluorescence Turn-On Analysis of Antiepileptic Drug Tiagabine Hydrochloride. Analytical chemistry. 2020 03; 92(5):3555-3562. doi: 10.1021/acs.analchem.9b03507. [PMID: 32008316]
  • Paula Zaręba, Beata Gryzło, Katarzyna Malawska, Kinga Sałat, Georg C Höfner, Alicja Nowaczyk, Łukasz Fijałkowski, Anna Rapacz, Adrian Podkowa, Anna Furgała, Paweł Żmudzki, Klaus T Wanner, Barbara Malawska, Katarzyna Kulig. Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice. European journal of medicinal chemistry. 2020 Feb; 188(?):111920. doi: 10.1016/j.ejmech.2019.111920. [PMID: 31901745]
  • Joonseon Yoon, Yunjung Han, Young Ock Ahn, Myoung-Ki Hong, Soon-Kee Sung. Characterization of HemY-type protoporphyrinogen IX oxidase genes from cyanobacteria and their functioning in transgenic Arabidopsis. Plant molecular biology. 2019 Dec; 101(6):561-574. doi: 10.1007/s11103-019-00925-8. [PMID: 31621006]
  • Katarzyna Socała, Elżbieta Wyska, Małgorzata Szafarz, Dorota Nieoczym, Piotr Wlaź. Acute effect of cannabidiol on the activity of various novel antiepileptic drugs in the maximal electroshock- and 6 Hz-induced seizures in mice: Pharmacodynamic and pharmacokinetic studies. Neuropharmacology. 2019 11; 158(?):107733. doi: 10.1016/j.neuropharm.2019.107733. [PMID: 31377197]
  • Simone K Huber, Georg Höfner, Klaus T Wanner. Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1). Bioorganic & medicinal chemistry. 2019 07; 27(13):2753-2763. doi: 10.1016/j.bmc.2019.05.001. [PMID: 31097402]
  • Felix Kern, Klaus T Wanner. Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1. Bioorganic & medicinal chemistry. 2019 04; 27(7):1232-1245. doi: 10.1016/j.bmc.2019.02.015. [PMID: 30777661]
  • Krisztián Tóth, Georg Höfner, Klaus T Wanner. Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors. Bioorganic & medicinal chemistry. 2019 03; 27(5):822-831. doi: 10.1016/j.bmc.2019.01.024. [PMID: 30718063]
  • Alicja Nowaczyk, Łukasz Fijałkowski, Magdalena Kowalska, Adrian Podkowa, Kinga Sałat. Studies on the Activity of Selected Highly Lipophilic Compounds toward hGAT1 Inhibition. Part II. ACS chemical neuroscience. 2019 01; 10(1):337-347. doi: 10.1021/acschemneuro.8b00282. [PMID: 30222312]
  • Tobias J Hauke, Georg Höfner, Klaus T Wanner. Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4. Bioorganic & medicinal chemistry. 2019 01; 27(1):144-152. doi: 10.1016/j.bmc.2018.11.028. [PMID: 30503411]
  • Alexandra R Sowa, Allen F Brooks, Xia Shao, Bradford D Henderson, Philip Sherman, Janna Arteaga, Jenelle Stauff, Adam C Lee, Robert A Koeppe, Peter J H Scott, Michael R Kilbourn. Development of Positron Emission Tomography Radiotracers for the GABA Transporter 1. ACS chemical neuroscience. 2018 11; 9(11):2767-2773. doi: 10.1021/acschemneuro.8b00183. [PMID: 29763549]
  • Tobias J Hauke, Thomas Wein, Georg Höfner, Klaus T Wanner. Novel Allosteric Ligands of γ-Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries. Journal of medicinal chemistry. 2018 11; 61(22):10310-10332. doi: 10.1021/acs.jmedchem.8b01602. [PMID: 30376325]
  • Krisztián Tóth, Georg Höfner, Klaus T Wanner. Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors. Bioorganic & medicinal chemistry. 2018 07; 26(12):3668-3687. doi: 10.1016/j.bmc.2018.05.049. [PMID: 29886082]
  • Shuwei Ning, Qiaozhen Kang, Dandan Fan, Jingjing Liu, Chaoyue Xue, Xiaolin Zhang, Cong Ding, Jianying Zhang, Qian Peng, Zhenyu Ji. Protein 4.1R is Involved in the Transport of 5-Aminolevulinic Acid by Interaction with GATs in MEF Cells. Photochemistry and photobiology. 2018 01; 94(1):173-178. doi: 10.1111/php.12842. [PMID: 28881432]
  • Ankit Seth, Piyoosh A Sharma, Avanish Tripathi, Priyanka K Choubey, Pavan Srivastava, Prabhash N Tripathi, Sushant K Shrivastava. Design, Synthesis, Evaluation and Computational Studies of Nipecotic Acid-Acetonaphthone Hybrids as Potential Antiepileptic Agents. Medicinal chemistry (Shariqah (United Arab Emirates)). 2018; 14(4):409-426. doi: 10.2174/1573406414666180116104225. [PMID: 29336266]
  • Giorgia Fattorini, Marcello Melone, María Victoria Sánchez-Gómez, Rogelio O Arellano, Silvia Bassi, Carlos Matute, Fiorenzo Conti. GAT-1 mediated GABA uptake in rat oligodendrocytes. Glia. 2017 03; 65(3):514-522. doi: 10.1002/glia.23108. [PMID: 28071826]
  • Arne Schousboe, Petrine Wellendorph, Bente Frølund, Rasmus P Clausen, Povl Krogsgaard-Larsen. Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs. Advances in neurobiology. 2017; 16(?):283-296. doi: 10.1007/978-3-319-55769-4_14. [PMID: 28828616]
  • Łukasz Fijałkowski, Kinga Sałat, Adrian Podkowa, Paula Zaręba, Alicja Nowaczyk. Potential role of selected antiepileptics used in neuropathic pain as human GABA transporter isoform 1 (GAT1) inhibitors-Molecular docking and pharmacodynamic studies. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2017 Jan; 96(?):362-372. doi: 10.1016/j.ejps.2016.10.004. [PMID: 27721044]
  • Jarogniew J Luszczki, Pawel Patrzylas, Miroslaw Zagaja, Marta Andres-Mach, Katarzyna Zaluska, Maria W Kondrat-Wrobel, Monika Szpringer, Jaroslaw Chmielewski, Magdalena Florek-Luszczki. Effects of arachidonyl-2'-chloroethylamide (ACEA) on the protective action of various antiepileptic drugs in the 6-Hz corneal stimulation model in mice. PloS one. 2017; 12(8):e0183873. doi: 10.1371/journal.pone.0183873. [PMID: 28859122]
  • Marwa Y Sallam, Sahar M El-Gowilly, Abdel-Galil A Abdel-Galil, Mahmoud M El-Mas. Central GABAA receptors are involved in inflammatory and cardiovascular consequences of endotoxemia in conscious rats. Naunyn-Schmiedeberg's archives of pharmacology. 2016 Mar; 389(3):279-88. doi: 10.1007/s00210-015-1201-7. [PMID: 26685896]
  • W Gordon Frankle, Raymond Y Cho, Konasale M Prasad, N Scott Mason, Jennifer Paris, Michael L Himes, Christopher Walker, David A Lewis, Rajesh Narendran. In vivo measurement of GABA transmission in healthy subjects and schizophrenia patients. The American journal of psychiatry. 2015 Nov; 172(11):1148-59. doi: 10.1176/appi.ajp.2015.14081031. [PMID: 26133962]
  • Jie Liu, Dongping Huang, Jing Xu, Jiabin Tong, Zishan Wang, Li Huang, Yufang Yang, Xiaochen Bai, Pan Wang, Haiyun Suo, Yuanyuan Ma, Mei Yu, Jian Fei, Fang Huang. Tiagabine Protects Dopaminergic Neurons against Neurotoxins by Inhibiting Microglial Activation. Scientific reports. 2015 Oct; 5(?):15720. doi: 10.1038/srep15720. [PMID: 26499517]
  • Kinga Sałat, Adrian Podkowa, Paula Kowalczyk, Katarzyna Kulig, Anna Dziubina, Barbara Filipek, Tadeusz Librowski. Anticonvulsant active inhibitor of GABA transporter subtype 1, tiagabine, with activity in mouse models of anxiety, pain and depression. Pharmacological reports : PR. 2015 Jun; 67(3):465-72. doi: 10.1016/j.pharep.2014.11.003. [PMID: 25933955]
  • Stine B Vogensen, Lars Jørgensen, Karsten K Madsen, Andreas Jurik, Nrupa Borkar, Emiliano Rosatelli, Birgitte Nielsen, Gerhard F Ecker, Arne Schousboe, Rasmus P Clausen. Structure activity relationship of selective GABA uptake inhibitors. Bioorganic & medicinal chemistry. 2015 May; 23(10):2480-8. doi: 10.1016/j.bmc.2015.03.060. [PMID: 25882526]
  • Tobias Steffan, Thejavathi Renukappa-Gutke, Georg Höfner, Klaus T Wanner. Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids. Bioorganic & medicinal chemistry. 2015 Mar; 23(6):1284-306. doi: 10.1016/j.bmc.2015.01.035. [PMID: 25698617]
  • Andreas Jurik, Barbara Zdrazil, Marion Holy, Thomas Stockner, Harald H Sitte, Gerhard F Ecker. A binding mode hypothesis of tiagabine confirms liothyronine effect on γ-aminobutyric acid transporter 1 (GAT1). Journal of medicinal chemistry. 2015 Mar; 58(5):2149-58. doi: 10.1021/jm5015428. [PMID: 25679268]
  • Shaza Deeb, Denise A McKeown, Hazel J Torrance, Fiona M Wylie, Barry K Logan, Karen S Scott. Simultaneous analysis of 22 antiepileptic drugs in postmortem blood, serum and plasma using LC-MS-MS with a focus on their role in forensic cases. Journal of analytical toxicology. 2014 Oct; 38(8):485-94. doi: 10.1093/jat/bku070. [PMID: 25217536]
  • James F M Myers, C John Evans, Nicola J Kalk, Richard A E Edden, Anne R Lingford-Hughes. Measurement of GABA using J-difference edited 1H-MRS following modulation of synaptic GABA concentration with tiagabine. Synapse (New York, N.Y.). 2014 Aug; 68(8):355-62. doi: 10.1002/syn.21747. [PMID: 24756906]
  • Masayuki Hiramatsu. [Functional role for GABA transporters in the CNS]. Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 2014 Apr; 143(4):187-92. doi: 10.1254/fpj.143.187. [PMID: 24717607]
  • Julie Marie V Timple, Lizandra Guidi Magalhães, Karen Cristina Souza Rezende, Ana Carolina Pereira, Wilson Roberto Cunha, Márcio Luis Andrade e Silva, Ole Valente Mortensen, Andréia C K Fontana. The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities. Journal of natural products. 2013 Oct; 76(10):1889-95. doi: 10.1021/np400452n. [PMID: 24112084]
  • Paula Kowalczyk, Kinga Sałat, Georg C Höfner, Natalia Guzior, Barbara Filipek, Klaus T Wanner, Katarzyna Kulig. 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. Bioorganic & medicinal chemistry. 2013 Sep; 21(17):5154-67. doi: 10.1016/j.bmc.2013.06.038. [PMID: 23859778]
  • Bolette Kragholm, Trine Kvist, Karsten K Madsen, Lars Jørgensen, Stine B Vogensen, Arne Schousboe, Rasmus P Clausen, Anders A Jensen, Hans Bräuner-Osborne. Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile. Biochemical pharmacology. 2013 Aug; 86(4):521-8. doi: 10.1016/j.bcp.2013.06.007. [PMID: 23792119]
  • Gabriele Quandt, Georg Höfner, Klaus T Wanner. Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors. Bioorganic & medicinal chemistry. 2013 Jun; 21(11):3363-78. doi: 10.1016/j.bmc.2013.02.056. [PMID: 23598250]
  • Suresh D Muthukumaraswamy, Jim F M Myers, Sue J Wilson, David J Nutt, Khalid Hamandi, Anne Lingford-Hughes, Krish D Singh. Elevating endogenous GABA levels with GAT-1 blockade modulates evoked but not induced responses in human visual cortex. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2013 May; 38(6):1105-12. doi: 10.1038/npp.2013.9. [PMID: 23361120]
  • Stine B Vogensen, Lars Jørgensen, Karsten K Madsen, Nrupa Borkar, Petrine Wellendorph, Jonas Skovgaard-Petersen, Arne Schousboe, H Steve White, Povl Krogsgaard-Larsen, Rasmus P Clausen. Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization. Journal of medicinal chemistry. 2013 Mar; 56(5):2160-4. doi: 10.1021/jm301872x. [PMID: 23398473]
  • Miriam Sindelar, Toni A Lutz, Marilena Petrera, Klaus T Wanner. Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1. Journal of medicinal chemistry. 2013 Feb; 56(3):1323-40. doi: 10.1021/jm301800j. [PMID: 23336362]
  • Olaf Schijns, Marinus van Kroonenburgh, Freek Beekman, Joost Verbeek, Jacobus Herscheid, Kim Rijkers, Veerle Visser-Vandewalle, Govert Hoogland. Development and characterization of [123I]iodotiagabine for in-vivo GABA-transporter imaging. Nuclear medicine communications. 2013 Feb; 34(2):175-9. doi: 10.1097/mnm.0b013e32835bbbd7. [PMID: 23187781]
  • Mai Shibata, Sachiyo Hashi, Haruka Nakanishi, Satohiro Masuda, Toshiya Katsura, Ikuko Yano. Detection of 22 antiepileptic drugs by ultra-performance liquid chromatography coupled with tandem mass spectrometry applicable to routine therapeutic drug monitoring. Biomedical chromatography : BMC. 2012 Dec; 26(12):1519-28. doi: 10.1002/bmc.2726. [PMID: 22383262]
  • László Héja, Gabriella Nyitrai, Orsolya Kékesi, Arpád Dobolyi, Pál Szabó, Richárd Fiáth, István Ulbert, Borbála Pál-Szenthe, Miklós Palkovits, Julianna Kardos. Astrocytes convert network excitation to tonic inhibition of neurons. BMC biology. 2012 Mar; 10(?):26. doi: 10.1186/1741-7007-10-26. [PMID: 22420899]
  • Søren Skovstrup, Laurent David, Olivier Taboureau, Flemming Steen Jørgensen. A steered molecular dynamics study of binding and translocation processes in the GABA transporter. PloS one. 2012; 7(6):e39360. doi: 10.1371/journal.pone.0039360. [PMID: 22737235]
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  • Kinga Sałat, Anna Więckowska, Krzysztof Więckowski, Georg C Höfner, Jacek Kamiński, Klaus T Wanner, Barbara Malawska, Barbara Filipek, Katarzyna Kulig. Synthesis and pharmacological properties of new GABA uptake inhibitors. Pharmacological reports : PR. 2012; 64(4):817-33. doi: 10.1016/s1734-1140(12)70877-0. [PMID: 23087134]
  • Karsten K Madsen, Bjarke Ebert, Rasmus P Clausen, Povl Krogsgaard-Larsen, Arne Schousboe, H Steve White. Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol. The Journal of pharmacology and experimental therapeutics. 2011 Jul; 338(1):214-9. doi: 10.1124/jpet.111.179671. [PMID: 21450931]
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