Tiagabine hydrochloride (BioDeep_00000015351)

   


代谢物信息卡片


Tiagabine hydrochloride

化学式: C20H26ClNO2S2 (411.10934060000005)
中文名称: 噻加宾盐酸盐
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CC1=C(SC=C1)C(=CCCN2CCCC(C2)C(=O)O)C3=C(C=CS3)C.Cl
InChI: /m1./s1

描述信息

D018377 - Neurotransmitter Agents > D014179 - Neurotransmitter Uptake Inhibitors > D058805 - GABA Uptake Inhibitors
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
Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively[1].

同义名列表

5 个代谢物同义名

Tiagabine hydrochloride; NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride; Tiagabine (hydrochloride)



数据库引用编号

8 个数据库交叉引用编号

分类词条

相关代谢途径

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代谢反应

0 个相关的代谢反应过程信息。

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INOH(0)

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  • 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。

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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]
  • 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]
  • 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]
  • 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]
  • 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]
  • 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]
  • 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]
  • 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]
  • 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]
  • 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]
  • 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]
  • Kazuaki Nakada, Mamie Yoshikawa, Soichiro Ide, Akihiro Suemasa, Shuhei Kawamura, Takaaki Kobayashi, Eiji Masuda, Yoshihiko Ito, Wataru Hayakawa, Takahiro Katayama, Shizuo Yamada, Mitsuhiro Arisawa, Masabumi Minami, Satoshi Shuto. Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports. Bioorganic & medicinal chemistry. 2013 Sep; 21(17):4938-50. doi: 10.1016/j.bmc.2013.06.063. [PMID: 23886812]
  • 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]
  • 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]
  • 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]
  • W Gordon Frankle, Raymond Y Cho, N Scott Mason, Chi-Min Chen, Michael Himes, Christopher Walker, David A Lewis, Chester A Mathis, Rajesh Narendran. [11C]flumazenil binding is increased in a dose-dependent manner with tiagabine-induced elevations in GABA levels. PloS one. 2012; 7(2):e32443. doi: 10.1371/journal.pone.0032443. [PMID: 22384252]
  • 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]
  • 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]
  • Aimin Tan, Isabelle A Lévesque, Isabelle M Lévesque, François Viel, Nadine Boudreau, Ann Lévesque. Analyte and internal standard cross signal contributions and their impact on quantitation in LC-MS based bioanalysis. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2011 Jul; 879(21):1954-60. doi: 10.1016/j.jchromb.2011.05.027. [PMID: 21680265]
  • A C Lehre, N M Rowley, Y Zhou, S Holmseth, C Guo, T Holen, R Hua, P Laake, A M Olofsson, I Poblete-Naredo, D A Rusakov, K K Madsen, R P Clausen, A Schousboe, H S White, N C Danbolt. Deletion of the betaine-GABA transporter (BGT1; slc6a12) gene does not affect seizure thresholds of adult mice. Epilepsy research. 2011 Jun; 95(1-2):70-81. doi: 10.1016/j.eplepsyres.2011.02.014. [PMID: 21459558]
  • Wolfgang Froestl. An historical perspective on GABAergic drugs. Future medicinal chemistry. 2011 Feb; 3(2):163-75. doi: 10.4155/fmc.10.285. [PMID: 21428811]
  • C Suñol, Z Babot, R Cristòfol, U Sonnewald, H S Waagepetersen, A Schousboe. A possible role of the non-GAT1 GABA transporters in transfer of GABA from GABAergic to glutamatergic neurons in mouse cerebellar neuronal cultures. Neurochemical research. 2010 Sep; 35(9):1384-90. doi: 10.1007/s11064-010-0196-1. [PMID: 20512624]
  • Søren Skovstrup, Olivier Taboureau, Hans Bräuner-Osborne, Flemming Steen Jørgensen. Homology modelling of the GABA transporter and analysis of tiagabine binding. ChemMedChem. 2010 Jul; 5(7):986-1000. doi: 10.1002/cmdc.201000100. [PMID: 20491137]
  • C K Thoeringer, A Erhardt, I Sillaber, M B Mueller, F Ohl, F Holsboer, M E Keck. Long-term anxiolytic and antidepressant-like behavioural effects of tiagabine, a selective GABA transporter-1 (GAT-1) inhibitor, coincide with a decrease in HPA system activity in C57BL/6 mice. Journal of psychopharmacology (Oxford, England). 2010 May; 24(5):733-43. doi: 10.1177/0269881109103091. [PMID: 19346277]
  • Jason G Meisner, Adam D Marsh, Daniel R Marsh. Loss of GABAergic interneurons in laminae I-III of the spinal cord dorsal horn contributes to reduced GABAergic tone and neuropathic pain after spinal cord injury. Journal of neurotrauma. 2010 Apr; 27(4):729-37. doi: 10.1089/neu.2009.1166. [PMID: 20059302]
  • Danièle Bentué-Ferrer, Olivier Tribut, Marie-Clémence Verdier. [Therapeutic drug monitoring of tiagabine]. Therapie. 2010 Jan; 65(1):51-5. doi: 10.2515/therapie/2009065. [PMID: 20205996]
  • Magdalena Chrościńska-Krawczyk, Neville Ratnaraj, Philip N Patsalos, Stanisław J Czuczwar. Effect of caffeine on the anticonvulsant effects of oxcarbazepine, lamotrigine and tiagabine in a mouse model of generalized tonic-clonic seizures. Pharmacological reports : PR. 2009 Sep; 61(5):819-26. doi: 10.1016/s1734-1140(09)70137-9. [PMID: 19904004]
  • Karsten K Madsen, Rasmus P Clausen, Orla M Larsson, Povl Krogsgaard-Larsen, Arne Schousboe, H Steve White. Synaptic and extrasynaptic GABA transporters as targets for anti-epileptic drugs. Journal of neurochemistry. 2009 May; 109 Suppl 1(?):139-44. doi: 10.1111/j.1471-4159.2009.05982.x. [PMID: 19393020]
  • Aaron H Burstein, Eilis A Boudreau, William H Theodore. Increase in tiagabine serum concentration with coadministration of gemfibrozil. The Annals of pharmacotherapy. 2009 Feb; 43(2):379-82. doi: 10.1345/aph.1l080. [PMID: 19193595]
  • W Gordon Frankle, Raymond Y Cho, Rajesh Narendran, N Scott Mason, Shivangi Vora, Maralee Litschge, Julie C Price, David A Lewis, Chester A Mathis. Tiagabine increases [11C]flumazenil binding in cortical brain regions in healthy control subjects. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2009 Feb; 34(3):624-33. doi: 10.1038/npp.2008.104. [PMID: 18615011]
  • Jarogniew J Luszczki. Interactions of tiagabine with ethosuximide in the mouse pentylenetetrazole-induced seizure model: an isobolographic analysis for non-parallel dose-response relationship curves. Naunyn-Schmiedeberg's archives of pharmacology. 2008 Nov; 378(5):483-92. doi: 10.1007/s00210-008-0305-8. [PMID: 18566800]
  • Naoki Masuda, Qi Peng, Qing Li, Mali Jiang, Yideng Liang, Xiaofang Wang, Ming Zhao, Wenfei Wang, Christopher A Ross, Wenzhen Duan. Tiagabine is neuroprotective in the N171-82Q and R6/2 mouse models of Huntington's disease. Neurobiology of disease. 2008 Jun; 30(3):293-302. doi: 10.1016/j.nbd.2008.01.014. [PMID: 18395459]
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