Tiagabine (BioDeep_00000406040)
Main id: BioDeep_00000002678
Volatile Flavor Compounds
代谢物信息卡片
Tiagabine
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 () 0%
分子结构信息
SMILES: CC1=C(SC=C1)C(=CCCN2CCCC(C2)C(=O)O)C3=C(C=CS3)C
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
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
数据库引用编号
17 个数据库交叉引用编号
- ChEBI: CHEBI:9586
- KEGG: C07503
- KEGGdrug: D08588
- PubChem: 60648
- DrugBank: DB00906
- ChEMBL: CHEMBL1027
- MeSH: Tiagabine
- CAS: 1006863-69-9
- CAS: 115103-54-3
- MoNA: FiehnHILIC003013
- MoNA: FiehnHILIC002362
- MoNA: FiehnHILIC000797
- PubChem: 9706
- PDB-CCD: TGI
- NIKKAJI: J390.632I
- RefMet: Tiagabine
- KNApSAcK: 9586
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)
0 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] - Caroline Nothdurfter, Rainer Rupprecht, Gerhard Rammes. Recent developments in potential anxiolytic agents targeting GABAA/BzR complex or the translocator protein (18kDa) (TSPO).
Current topics in medicinal chemistry.
2012; 12(4):360-70. doi:
10.2174/156802612799078748. [PMID: 22204486] - Gerile, Chiharu Sogawa, Kazumi Ohyama, Takashi Masuko, Tadashi Kusama, Katsuya Morita, Norio Sogawa, Shigeo Kitayama. Inhibitory action of antidepressants on mouse Betaine/GABA transporter (BGT1) heterologously expressed in cell cultures.
International journal of molecular sciences.
2012; 13(3):2578-2589. doi:
10.3390/ijms13032578. [PMID: 22489112] - 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] - Slobodan M Jankovic, Milivoje Dostic. Choice of antiepileptic drugs for the elderly: possible drug interactions and adverse effects.
Expert opinion on drug metabolism & toxicology.
2012 Jan; 8(1):81-91. doi:
10.1517/17425255.2012.645535. [PMID: 22175232] - 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] - 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] - Sonja Sucic, Ali El-Kasaby, Oliver Kudlacek, Subhodeep Sarker, Harald H Sitte, Philippe Marin, Michael Freissmuth. The serotonin transporter is an exclusive client of the coat protein complex II (COPII) component SEC24C.
The Journal of biological chemistry.
2011 May; 286(18):16482-90. doi:
10.1074/jbc.m111.230037. [PMID: 21454670] - Arne Schousboe, Karsten K Madsen, H Steve White. GABA transport inhibitors and seizure protection: the past and future.
Future medicinal chemistry.
2011 Feb; 3(2):183-7. doi:
10.4155/fmc.10.288. [PMID: 21428813] - Howard N Bockbrader, Paula Burger, Lloyd Knapp. Pregabalin effect on steady-state pharmacokinetics of carbamazepine, lamotrigine, phenobarbital, phenytoin, topiramate, valproate, and tiagabine.
Epilepsia.
2011 Feb; 52(2):405-9. doi:
10.1111/j.1528-1167.2010.02763.x. [PMID: 21314678] - 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] - B Mishra, B L Sahoo, M Mishra, D Shukla, V Kumar. Design of a controlled release liquid formulation of lamotrigine.
Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences.
2011; 19(2):126-37. doi:
NULL. [PMID: 22615649] - Domenica A Pizzi, Colin P Leslie, Romano Di Fabio, Catia Seri, Giovanni Bernasconi, Michela Squaglia, Gennaro Carnevale, Alessandro Falchi, Elisabetta Greco, Laura Mangiarini, Michele Negri. Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.
Bioorganic & medicinal chemistry letters.
2011 Jan; 21(1):602-5. doi:
10.1016/j.bmcl.2010.09.025. [PMID: 21134748] - Muhannad R M Salih, Mohd Baidi Bahari, Arwa Y Abd. Selected pharmacokinetic issues of the use of antiepileptic drugs and parenteral nutrition in critically ill patients.
Nutrition journal.
2010 Dec; 9(?):71. doi:
10.1186/1475-2891-9-71. [PMID: 21194458] - Iiris Sorri, Mitchell G Brigell, Miklos Mályusz, Eija Mahlamäki, Capucine de Meynard, Reetta Kälviäinen. Is reduced ornithine-δ-aminotransferase activity the cause of vigabatrin-associated visual field defects?.
Epilepsy research.
2010 Nov; 92(1):48-53. doi:
10.1016/j.eplepsyres.2010.08.006. [PMID: 20850272] - Svein I Johannessen, Cecilie Johannessen Landmark. Antiepileptic drug interactions - principles and clinical implications.
Current neuropharmacology.
2010 Sep; 8(3):254-67. doi:
10.2174/157015910792246254. [PMID: 21358975] - 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] - Joel S Goldberg. Selected Gamma Aminobutyric Acid (GABA) Esters may Provide Analgesia for Some Central Pain Conditions.
Perspectives in medicinal chemistry.
2010 Aug; 4(?):23-31. doi:
10.4137/pmc.s5490. [PMID: 20703328] - 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] - Mark R Faust, Georg Höfner, Jörg Pabel, Klaus T Wanner. Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.
European journal of medicinal chemistry.
2010 Jun; 45(6):2453-66. doi:
10.1016/j.ejmech.2010.02.029. [PMID: 20219271] - 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] - Karsten K Madsen, H Steve White, Arne Schousboe. Neuronal and non-neuronal GABA transporters as targets for antiepileptic drugs.
Pharmacology & therapeutics.
2010 Mar; 125(3):394-401. doi:
10.1016/j.pharmthera.2009.11.007. [PMID: 20026354] - J Kardos, A Palló, A Bencsura, A Simon. Assessing structure, function and druggability of major inhibitory neurotransmitter gamma-aminobutyrate symporter subtypes.
Current medicinal chemistry.
2010; 17(20):2203-13. doi:
10.2174/092986710791299939. [PMID: 20423300] - Cynthia M Anderson, Patrick D Kidd, Sepehr Eskandari. GATMD: γ-aminobutyric acid transporter mutagenesis database.
Database : the journal of biological databases and curation.
2010; 2010(?):baq028. doi:
10.1093/database/baq028. [PMID: 21131297] - 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] - László Héja, Péter Barabás, Gabriella Nyitrai, Katalin A Kékesi, Bálint Lasztóczi, Orsolya Toke, Gábor Tárkányi, Karsten Madsen, Arne Schousboe, Arpád Dobolyi, Miklós Palkovits, Julianna Kardos. Glutamate uptake triggers transporter-mediated GABA release from astrocytes.
PloS one.
2009 Sep; 4(9):e7153. doi:
10.1371/journal.pone.0007153. [PMID: 19777062] - K K Akula, A Dhir, S K Kulkarni. Effect of various antiepileptic drugs in a pentylenetetrazol-induced seizure model in mice.
Methods and findings in experimental and clinical pharmacology.
2009 Sep; 31(7):423-32. doi:
10.1358/mf.2009.31.7.1393610. [PMID: 19907717] - 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] - S Arpin, E Lagrue, S Bodard, S Chalon, P Castelnau. Basal ganglia neuroprotection with anticonvulsants after energy stress: a comparative study.
Metabolic brain disease.
2009 Sep; 24(3):453-61. doi:
10.1007/s11011-009-9144-7. [PMID: 19789969] - Manthena V S Varma, Bo Feng, R Scott Obach, Matthew D Troutman, Jonathan Chupka, Howard R Miller, Ayman El-Kattan. Physicochemical determinants of human renal clearance.
Journal of medicinal chemistry.
2009 Aug; 52(15):4844-52. doi:
10.1021/jm900403j. [PMID: 19445515] - C K Thoeringer, S Ripke, P G Unschuld, S Lucae, M Ising, T Bettecken, M Uhr, M E Keck, B Mueller-Myhsok, F Holsboer, E B Binder, A Erhardt. The GABA transporter 1 (SLC6A1): a novel candidate gene for anxiety disorders.
Journal of neural transmission (Vienna, Austria : 1996).
2009 Jun; 116(6):649-57. doi:
10.1007/s00702-008-0075-y. [PMID: 18607529] - 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] - Martin E Duddy, Mark R Baker. Stiff person syndrome.
Frontiers of neurology and neuroscience.
2009; 26(?):147-165. doi:
10.1159/000212375. [PMID: 19349711] - Pamela M Crawford. Managing epilepsy in women of childbearing age.
Drug safety.
2009; 32(4):293-307. doi:
10.2165/00002018-200932040-00004. [PMID: 19388721] - 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] - Andrea Kragler, Georg Höfner, Klaus T Wanner. Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.
European journal of medicinal chemistry.
2008 Nov; 43(11):2404-11. doi:
10.1016/j.ejmech.2008.01.005. [PMID: 18395300] - C M Tartaglione, M N Ritta. On the presence of 3H-GABA uptake mechanism in bovine spermatozoa.
Animal reproduction science.
2008 Oct; 108(1-2):247-58. doi:
10.1016/j.anireprosci.2007.08.010. [PMID: 17954017] - Karl O Nakken, Svein I Johannessen. [Seizure exacerbation caused by antiepileptic drugs].
Tidsskrift for den Norske laegeforening : tidsskrift for praktisk medicin, ny raekke.
2008 Sep; 128(18):2052-5. doi:
. [PMID: 18846119] - Kevin Yi-Lwern Yap, Wai Keung Chui, Alexandre Chan. Drug interactions between chemotherapeutic regimens and antiepileptics.
Clinical therapeutics.
2008 Aug; 30(8):1385-407. doi:
10.1016/j.clinthera.2008.08.011. [PMID: 18803983] - R Scott Obach, Franco Lombardo, Nigel J Waters. Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Drug metabolism and disposition: the biological fate of chemicals.
2008 Jul; 36(7):1385-405. doi:
10.1124/dmd.108.020479. [PMID: 18426954] - 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] - K K Borowicz, M Zadrozniak, J J Luszczki, S J Czuczwar. Interactions between tiagabine and conventional antiepileptic drugs in the rat model of complex partial seizures.
Journal of neural transmission (Vienna, Austria : 1996).
2008 May; 115(5):661-7. doi:
10.1007/s00702-007-0006-3. [PMID: 18193378] - L M McDonald, W F Sheppard, S M Staveley, B Sohal, F D Tattersall, P H Hutson. Discriminative stimulus effects of tiagabine and related GABAergic drugs in rats.
Psychopharmacology.
2008 May; 197(4):591-600. doi:
10.1007/s00213-008-1077-z. [PMID: 18264695] - Ashish Dhir, Kiran Kumar Akula, S K Kulkarni. Tiagabine, a GABA uptake inhibitor, attenuates 3-nitropropionic acid-induced alterations in various behavioral and biochemical parameters in rats.
Progress in neuro-psychopharmacology & biological psychiatry.
2008 Apr; 32(3):835-43. doi:
10.1016/j.pnpbp.2007.12.017. [PMID: 18234412] - J Pistovcakova, M Dostalek, A Sulcova, D Jezova. Tiagabine treatment is associated with neurochemical, immune and behavioural alterations in the olfactory bulbectomized rat model of depression.
Pharmacopsychiatry.
2008 Mar; 41(2):54-9. doi:
10.1055/s-2007-993212. [PMID: 18311685] - Misty D Smith, Gerald W Saunders, Rasmus P Clausen, Bente Frølund, Povl Krogsgaard-Larsen, Orla M Larsson, Arne Schousboe, Karen S Wilcox, H Steve White. Inhibition of the betaine-GABA transporter (mGAT2/BGT-1) modulates spontaneous electrographic bursting in the medial entorhinal cortex (mEC).
Epilepsy research.
2008 Mar; 79(1):6-13. doi:
10.1016/j.eplepsyres.2007.12.009. [PMID: 18262393] - Yin Fang Xu, You Qing Cai, Guo Qiang Cai, Jie Jiang, Zhe Jing Sheng, Zhu Gang Wang, Jian Fei. Hypoalgesia in mice lacking GABA transporter subtype 1.
Journal of neuroscience research.
2008 Feb; 86(2):465-70. doi:
10.1002/jnr.21499. [PMID: 17918738] - Agnieszka Basta-Kaim, Bogusława Budziszewska, Władysław Lasoń. [Effects of antiepileptic drugs on immune system].
Przeglad lekarski.
2008; 65(11):799-802. doi:
. [PMID: 19205364] - Bernhard J Steinhoff. Pregnancy, epilepsy, and anticonvulsants.
Dialogues in clinical neuroscience.
2008; 10(1):63-75. doi:
NULL. [PMID: 18472485] - Theresa Winhusen, Eugene Somoza, Domenic A Ciraulo, Judy M Harrer, R Jeffrey Goldsmith, John Grabowski, Florence S Coleman, Gordon Mindrum, Roberta Kahn, Sabuhi Osman, Juris Mezinskis, Shou-Hua Li, Daniel Lewis, Paul Horn, Margaret A Montgomery, Ahmed Elkashef. A double-blind, placebo-controlled trial of tiagabine for the treatment of cocaine dependence.
Drug and alcohol dependence.
2007 Dec; 91(2-3):141-8. doi:
10.1016/j.drugalcdep.2007.05.028. [PMID: 17629631] - Rungnapa Hirunsatit, Risto Ilomäki, Robert Malison, Pirkko Räsänen, Essi Ilomäki, Henry R Kranzler, Thomas Kosten, Atapol Sughondhabirom, Nuntika Thavichachart, Sookjaroen Tangwongchai, Jennifer Listman, Apiwat Mutirangura, Joel Gelernter, Jaakko Lappalainen. Sequence variation and linkage disequilibrium in the GABA transporter-1 gene (SLC6A1) in five populations: implications for pharmacogenetic research.
BMC genetics.
2007 Oct; 8(?):71. doi:
10.1186/1471-2156-8-71. [PMID: 17941974] - Yinfang Xu, Youqing Cai, Neng Gong, Chen Chen, Yuncheng Wu, Sandy Zhang-Nunes, Zhugang Wang, Tianle Xu, Jian Fei. Homeostatic plasticity of GABAergic synaptic transmission in mice lacking GAT1.
Biochemical and biophysical research communications.
2007 Sep; 361(2):499-504. doi:
10.1016/j.bbrc.2007.07.042. [PMID: 17655829] - Jiange Zhang, Pei Zhang, Xianbo Liu, Kai Fang, Guoqiang Lin. Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors.
Bioorganic & medicinal chemistry letters.
2007 Jul; 17(13):3769-73. doi:
10.1016/j.bmcl.2007.04.010. [PMID: 17517506]