Riluzole (BioDeep_00000003173)

human metabolite blood metabolite Chemicals and Drugs

代谢物信息卡片

6-(trifluoromethoxy)-1,3-benzothiazol-2-amine

化学式: C8H5F3N2OS (234.00746759999998)
中文名称: 利鲁唑
谱图信息: 最多检出来源 Homo sapiens(blood) 68.42%

分子结构信息

SMILES: C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N
InChI: InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13)

描述信息

Riluzole is only found in individuals that have used or taken this drug. It is a glutamate antagonist (receptors, glutamate) used as an anticonvulsant (anticonvulsants) and to prolong the survival of patients with amyotrophic lateral sclerosis. [PubChem]The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release (activation of glutamate reuptake), 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors.
D018377 - Neurotransmitter Agents > D018683 - Excitatory Amino Acid Agents > D018691 - Excitatory Amino Acid Antagonists
D002491 - Central Nervous System Agents > D018696 - Neuroprotective Agents
C78272 - Agent Affecting Nervous System > C264 - Anticonvulsant Agent
D002491 - Central Nervous System Agents > D000927 - Anticonvulsants
D020011 - Protective Agents
N - Nervous system
Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.

同义名列表

13 个代谢物同义名

6-(trifluoromethoxy)-1,3-benzothiazol-2-amine; 2 Amino 6 trifluoromethoxybenzothiazole; 2-Amino-6-trifluoromethoxybenzothiazole; Rhone poulenc rorer brand OF riluzole; Rhone-poulenc rorer brand OF riluzole; Aventis behring brand OF riluzole; Aventis brand OF riluzole; Impax brand OF riluzole; Riluzole aventis brand; Riluzole impax brand; riluzole; Rilutek; PK 26124

数据库引用编号

18 个数据库交叉引用编号

ChEBI: CHEBI:8863
KEGG: C07937
KEGGdrug: D00775
PubChem: 5070
HMDB: HMDB0014878
Metlin: METLIN2321
DrugBank: DB00740
ChEMBL: CHEMBL744
Wikipedia: Riluzole
MeSH: Riluzole
chemspider: 4892
CAS: 1744-22-5
PMhub: MS000008379
PubChem: 10139
PDB-CCD: 657
NIKKAJI: J22.921K
RefMet: Riluzole
medchemexpress: HY-B0211

分类词条

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

9606 Homo sapiens: -

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

Ruifen Cai, Juan Yang, Lijuan Wu, Yixiao Liu, Xinrui Wang, Qingshan Zheng, Lujin Li. Accelerating drug development for amyotrophic lateral sclerosis: construction and application of a disease course model using historical placebo group data. Orphanet journal of rare diseases. 2024 Feb; 19(1):40. doi: 10.1186/s13023-024-03057-5. [PMID: 38308282]
Maria A Lapshina, Elena F Shevtsova, Vladimir V Grigoriev, Aleksey Yu Aksinenko, Aleksey A Ustyugov, Daniil A Steinberg, Grigoriy V Maleev, Elena S Dubrovskaya, Tatiana V Goreva, Tatiana A Epishina, Vladimir L Zamoyski, Galina F Makhaeva, Vladimir P Fisenko, Ivan M Veselov, Daria V Vinogradova, Sergey O Bachurin. New Adamantane-Containing Edaravone Conjugates as Potential Neuroprotective Agents for ALS Treatments. Molecules (Basel, Switzerland). 2023 Nov; 28(22):. doi: 10.3390/molecules28227567. [PMID: 38005288]
Xavier Llorente, Gerard Esteruelas, Lorena Bonilla, Mariana Garnica Agudelo, Ingrid Filgaira, Daniel Lopez-Ramajo, Ruoyi C Gong, Concepció Soler, Marta Espina, Maria Luisa García, Joan Manils, Montserrat Pujol, Elena Sánchez-López. Riluzole-Loaded Nanostructured Lipid Carriers for Hyperproliferative Skin Diseases. International journal of molecular sciences. 2023 Apr; 24(9):. doi: 10.3390/ijms24098053. [PMID: 37175765]
Lucas Matheus Gonçalves de Oliveira, Rodrigo Barreto Carreira, Juciele Valeria Ribeiro de Oliveira, Ravena Pereira do Nascimento, Cleide Dos Santos Souza, Emiliano Trias, Victor Diogenes Amaral da Silva, Silvia Lima Costa. Impact of Plant-Derived Compounds on Amyotrophic Lateral Sclerosis. Neurotoxicity research. 2023 Feb; ?(?):. doi: 10.1007/s12640-022-00632-1. [PMID: 36800114]
Sumra Malik, G A Miana, Athar Ata, Madiha Kanwal, Saima Maqsood, Imran Malik, Zartashia Kazmi. Synthesis, characterization, in-silico, and pharmacological evaluation of new 2-amino-6‑trifluoromethoxy benzothiazole derivatives. Bioorganic chemistry. 2023 01; 130(?):106175. doi: 10.1016/j.bioorg.2022.106175. [PMID: 36410112]
Lin Yang, Qiuting Ren, Xu Ma, Mingwei Wang, Jinge Sun, Shen Wang, Xiaoyu Wu, Xinglin Chen, Chenxin Wang, Qingqing Li, Jinsheng Sun. New insight into the effect of riluzole on cadmium tolerance and accumulation in duckweed (Lemna turionifera). Ecotoxicology and environmental safety. 2022 Aug; 241(?):113783. doi: 10.1016/j.ecoenv.2022.113783. [PMID: 36068738]
Ann W Silk, Biren Saraiya, Roman Groisberg, Nancy Chan, Kristen Spencer, Eugenia Girda, Weichung Shih, Marisa Palmeri, Tracie Saunders, Robert M Berman, Vlad Coric, Suzie Chen, Andrew Zloza, Joshua Vieth, Janice M Mehnert, Jyoti Malhotra. A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors. European journal of medical research. 2022 Jul; 27(1):107. doi: 10.1186/s40001-022-00732-w. [PMID: 35780243]
Yi Deng, Rachel W Li, Yong Liang Yang, Steven Weiss, Paul N Smith. Pharmacological prevention of renal ischemia-reperfusion injury in a rat model. ANZ journal of surgery. 2022 03; 92(3):518-525. doi: 10.1111/ans.17381. [PMID: 34820987]
Tanja Dučić, Milena Ninkovic, Immaculada Martínez-Rovira, Swetlana Sperling, Veit Rohde, Dragoljub Dimitrijević, Gabriel Vicent Jover Mañas, Lisa Vaccari, Giovanni Birarda, Ibraheem Yousef. Live-Cell Synchrotron-Based FTIR Evaluation of Metabolic Compounds in Brain Glioblastoma Cell Lines after Riluzole Treatment. Analytical chemistry. 2022 02; 94(4):1932-1940. doi: 10.1021/acs.analchem.1c02076. [PMID: 34965097]
Mark J Henderson, Kathleen A Trychta, Shyh-Ming Yang, Susanne Bäck, Adam Yasgar, Emily S Wires, Carina Danchik, Xiaokang Yan, Hideaki Yano, Lei Shi, Kuo-Jen Wu, Amy Q Wang, Dingyin Tao, Gergely Zahoránszky-Kőhalmi, Xin Hu, Xin Xu, David Maloney, Alexey V Zakharov, Ganesha Rai, Fumihiko Urano, Mikko Airavaara, Oksana Gavrilova, Ajit Jadhav, Yun Wang, Anton Simeonov, Brandon K Harvey. A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. Cell reports. 2021 04; 35(4):109040. doi: 10.1016/j.celrep.2021.109040. [PMID: 33910017]
Mátyás C Földi, Krisztina Pesti, Katalin Zboray, Adam V Toth, Tamás Hegedűs, András Málnási-Csizmadia, Peter Lukacs, Arpad Mike. The mechanism of non-blocking inhibition of sodium channels revealed by conformation-selective photolabeling. British journal of pharmacology. 2021 03; 178(5):1200-1217. doi: 10.1111/bph.15365. [PMID: 33450052]
Nahit Rizaner, Sercan Uzun, Scott P Fraser, Mustafa B A Djamgoz, Seyhan Altun. Riluzole: Anti-invasive effects on rat prostate cancer cells under normoxic and hypoxic conditions. Basic & clinical pharmacology & toxicology. 2020 Oct; 127(4):254-264. doi: 10.1111/bcpt.13417. [PMID: 32304618]
Duygu Aydemir, Nuriye Nuray Ulusu. Importance of the serum biochemical parameters as potential biomarkers for rapid diagnosis and evaluating preclinical stage of ALS. Medical hypotheses. 2020 Aug; 141(?):109736. doi: 10.1016/j.mehy.2020.109736. [PMID: 32315925]
Irfan Qureshi, Meghan Lovegren, Victoria Wirtz, Richard Larouche, Mario Tanguay, Matt S Anderson, Sonja Hartmann, Vlad Coric, Robert M Berman. A Pharmacokinetic Bioequivalence Study Comparing Sublingual Riluzole (BHV-0223) and Oral Tablet Formulation of Riluzole in Healthy Volunteers. Clinical pharmacology in drug development. 2020 05; 9(4):476-485. doi: 10.1002/cpdd.747. [PMID: 31610101]
Benjamin Rix Brooks, Paolo Bettica, Sara Cazzaniga. Riluzole Oral Suspension: Bioavailability Following Percutaneous Gastrostomy Tube-modeled Administration Versus Direct Oral Administration. Clinical therapeutics. 2019 12; 41(12):2490-2499. doi: 10.1016/j.clinthera.2019.09.016. [PMID: 31635890]
Tobie D Lee, Olivia W Lee, Kyle R Brimacombe, Lu Chen, Rajarshi Guha, Sabrina Lusvarghi, Bethilehem G Tebase, Carleen Klumpp-Thomas, Robert W Robey, Suresh V Ambudkar, Min Shen, Michael M Gottesman, Matthew D Hall. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology. 2019 11; 96(5):629-640. doi: 10.1124/mol.119.115964. [PMID: 31515284]
Clément Ghiazza, Thierry Billard, Callum Dickson, Anis Tlili, Christian M Gampe. Chalcogen OCF3 Isosteres Modulate Drug Properties without Introducing Inherent Liabilities. ChemMedChem. 2019 09; 14(17):1586-1589. doi: 10.1002/cmdc.201900452. [PMID: 31364270]
Long-Yun Zhou, Zi-Rui Tian, Min Yao, Xu-Qing Chen, Yong-Jia Song, Jie Ye, Nan-Xing Yi, Xue-Jun Cui, Yong-Jun Wang. Riluzole promotes neurological function recovery and inhibits damage extension in rats following spinal cord injury: a meta-analysis and systematic review. Journal of neurochemistry. 2019 07; 150(1):6-27. doi: 10.1111/jnc.14686. [PMID: 30786027]
Mohammad-Hadi Farahzadi, Ehsan Moazen-Zadeh, Emran Razaghi, Mohammad-Reza Zarrindast, Reza Bidaki, Shahin Akhondzadeh. Riluzole for treatment of men with methamphetamine dependence: A randomized, double-blind, placebo-controlled clinical trial. Journal of psychopharmacology (Oxford, England). 2019 03; 33(3):305-315. doi: 10.1177/0269881118817166. [PMID: 30526230]
Ana P L Perdigão, Natalícia de Jesus Antunes, Lucas T Juni, Noedi L de Freitas, Julio Rojas-Moscoso, Sílvia V M Corrêa, Ronaldo C da Costa, Ronilson A Moreno, Gustavo D Mendes, Gilberto De Nucci. Pharmacokinetics of Riluzole in Beagle Dogs. Drug research. 2019 Jan; 69(1):40-45. doi: 10.1055/a-0645-1248. [PMID: 29991087]
Atyeh Rahimi, Saeed Nojavan. Electromembrane extraction of verapamil and riluzole from urine and wastewater samples using a mixture of organic solvents as a supported liquid membrane: Study on electric current variations. Journal of separation science. 2019 Jan; 42(2):566-573. doi: 10.1002/jssc.201800741. [PMID: 30371989]
Samuel T Wilkinson, Carly Kiselycznyk, Mounira Banasr, Ryan D Webler, Colin Haile, Sanjay J Mathew. Serum and plasma brain-derived neurotrophic factor and response in a randomized controlled trial of riluzole for treatment resistant depression. Journal of affective disorders. 2018 12; 241(?):514-518. doi: 10.1016/j.jad.2018.08.075. [PMID: 30153634]
Mahua Sarkar, Robert G Grossman, Elizabeth G Toups, Diana S-L Chow. Rational design and development of a stable liquid formulation of riluzole and its pharmacokinetic evaluation after oral and IV administrations in rats. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2018 Dec; 125(?):1-10. doi: 10.1016/j.ejps.2018.09.004. [PMID: 30201516]
Tianzhi Yang, Laine Ferrill, Leanne Gallant, Sarah McGillicuddy, Tatiana Fernandes, Nicole Schields, Shuhua Bai. Verapamil and riluzole cocktail liposomes overcome pharmacoresistance by inhibiting P-glycoprotein in brain endothelial and astrocyte cells: A potent approach to treat amyotrophic lateral sclerosis. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2018 Jul; 120(?):30-39. doi: 10.1016/j.ejps.2018.04.026. [PMID: 29704642]
Jeffrey C Pelletier, Suzie Chen, Haiyan Bian, Raj Shah, Garry R Smith, Jay E Wrobel, Allen B Reitz. Dipeptide Prodrugs of the Glutamate Modulator Riluzole. ACS medicinal chemistry letters. 2018 Jul; 9(7):752-756. doi: 10.1021/acsmedchemlett.8b00189. [PMID: 30034613]
Peter Lukacs, Mátyás C Földi, Luca Valánszki, Emilio Casanova, Beáta Biri-Kovács, László Nyitray, András Málnási-Csizmadia, Arpad Mike. Non-blocking modulation contributes to sodium channel inhibition by a covalently attached photoreactive riluzole analog. Scientific reports. 2018 05; 8(1):8110. doi: 10.1038/s41598-018-26444-y. [PMID: 29802266]
Sungha Kim, Jae Kyoun Kim, Mi Ju Son, Dongwoung Kim, Bongkeun Song, Ilhong Son, Hyung Won Kang, Jongdeok Lee, Sungchul Kim. Mecasin treatment in patients with amyotrophic lateral sclerosis: study protocol for a randomized controlled trial. Trials. 2018 Apr; 19(1):225. doi: 10.1186/s13063-018-2557-z. [PMID: 29653550]
Suzanne L Parker, Yarmarly C Guerra Valero, Jeffrey Lipman, Steven Weiss, Camilla Smith, Lyndal Russell, Paul Smith, Jason A Roberts, Steven C Wallis. A validated UHPLC-MS/MS method for the measurement of riluzole in plasma and myocardial tissue samples. Biomedical chromatography : BMC. 2017 Dec; 31(12):. doi: 10.1002/bmc.4030. [PMID: 28623867]
Paul Grant, Cristan Farmer, Jane Song, Timothy Kish, Susan Swedo. Riluzole Serum Concentration in Pediatric Patients Treated for Obsessive-Compulsive Disorder. Journal of clinical psychopharmacology. 2017 Dec; 37(6):713-716. doi: 10.1097/jcp.0000000000000797. [PMID: 29045303]
Jiayi Zhu, Lan Shen, Xiao Lin, Yanlong Hong, Yi Feng. Clinical Research on Traditional Chinese Medicine compounds and their preparations for Amyotrophic Lateral Sclerosis. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2017 Dec; 96(?):854-864. doi: 10.1016/j.biopha.2017.09.135. [PMID: 29078263]
Mahua Sarkar, Robert G Grossman, Elizabeth G Toups, Diana S-L Chow. UPLC-MS/MS assay of riluzole in human plasma and cerebrospinal fluid (CSF): Application in samples from spinal cord injured patients. Journal of pharmaceutical and biomedical analysis. 2017 Nov; 146(?):334-340. doi: 10.1016/j.jpba.2017.08.045. [PMID: 28917164]
Li Wan, Jiangjiang Bi, Jun Li, Zhiyi Zuo. Glutamate transporter type 3 participates in maintaining morphine-induced conditioned place preference. Neuroscience. 2017 03; 344(?):67-73. doi: 10.1016/j.neuroscience.2016.12.038. [PMID: 28049029]
Jens Kuhle, Bardia Nourbakhsh, Donna Grant, Steve Morant, Christian Barro, Özgür Yaldizli, Daniel Pelletier, Gavin Giovannoni, Emmanuelle Waubant, Sharmilee Gnanapavan. Serum neurofilament is associated with progression of brain atrophy and disability in early MS. Neurology. 2017 Feb; 88(9):826-831. doi: 10.1212/wnl.0000000000003653. [PMID: 28148632]
Cécile Brocard, Vanessa Plantier, Pascale Boulenguez, Sylvie Liabeuf, Mouloud Bouhadfane, Annelise Viallat-Lieutaud, Laurent Vinay, Frédéric Brocard. Cleavage of Na(+) channels by calpain increases persistent Na(+) current and promotes spasticity after spinal cord injury. Nature medicine. 2016 Apr; 22(4):404-11. doi: 10.1038/nm.4061. [PMID: 26974309]
Lili Wang, Jin Yan, Yaping Li, Kailin Xu, Shanshan Li, Peixiao Tang, Hui Li. The influence of hydroxypropyl-β-cyclodextrin on the solubility, dissolution, cytotoxicity, and binding of riluzole with human serum albumin. Journal of pharmaceutical and biomedical analysis. 2016 Jan; 117(?):453-63. doi: 10.1016/j.jpba.2015.09.033. [PMID: 26454338]
Patrick Türck, Marcos Emílio Frizzo. Riluzole stimulates BDNF release from human platelets. BioMed research international. 2015; 2015(?):189307. doi: 10.1155/2015/189307. [PMID: 25629040]
Yu Deng, Zhaofa Xu, Bin Xu, Wei Liu, Yangang Wei, Yuehui Li, Shu Feng, Tianyao Yang. Exploring cross-talk between oxidative damage and excitotoxicity and the effects of riluzole in the rat cortex after exposure to methylmercury. Neurotoxicity research. 2014 Jul; 26(1):40-51. doi: 10.1007/s12640-013-9448-6. [PMID: 24519665]
Fabiola Puentes, Joanne Topping, Jens Kuhle, Baukje J van der Star, Abdel Douiri, Gavin Giovannoni, David Baker, Sandra Amor, Andrea Malaspina. Immune reactivity to neurofilament proteins in the clinical staging of amyotrophic lateral sclerosis. Journal of neurology, neurosurgery, and psychiatry. 2014 Mar; 85(3):274-8. doi: 10.1136/jnnp-2013-305494. [PMID: 24078718]
Robert G Grossman, Michael G Fehlings, Ralph F Frankowski, Keith D Burau, Diana S L Chow, Charles Tator, Angela Teng, Elizabeth G Toups, James S Harrop, Bizhan Aarabi, Christopher I Shaffrey, Michele M Johnson, Susan J Harkema, Maxwell Boakye, James D Guest, Jefferson R Wilson. A prospective, multicenter, phase I matched-comparison group trial of safety, pharmacokinetics, and preliminary efficacy of riluzole in patients with traumatic spinal cord injury. Journal of neurotrauma. 2014 Feb; 31(3):239-55. doi: 10.1089/neu.2013.2969. [PMID: 23859435]
Holly M Brothers, Isabelle Bardou, Sarah C Hopp, Roxanne M Kaercher, Angela W Corona, Ashley M Fenn, Jonathan P Godbout, Gary L Wenk. Riluzole partially rescues age-associated, but not LPS-induced, loss of glutamate transporters and spatial memory. Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology. 2013 Dec; 8(5):1098-105. doi: 10.1007/s11481-013-9476-2. [PMID: 23709339]
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Bareket Daniel, Omer Green, Olga Viskind, Arie Gruzman. Riluzole increases the rate of glucose transport in L6 myotubes and NSC-34 motor neuron-like cells via AMPK pathway activation. Amyotrophic lateral sclerosis & frontotemporal degeneration. 2013 Sep; 14(5-6):434-43. doi: 10.3109/21678421.2013.808226. [PMID: 23834207]
Yongchao Wu, Kajana Satkunendrarajah, Yang Teng, Diana S-L Chow, Josef Buttigieg, Michael G Fehlings. Delayed post-injury administration of riluzole is neuroprotective in a preclinical rodent model of cervical spinal cord injury. Journal of neurotrauma. 2013 Mar; 30(6):441-52. doi: 10.1089/neu.2012.2622. [PMID: 23517137]
Punna Rao Ravi, Rahul Vats, Upendra Reddy Kora. Effect of ciprofloxacin and grapefruit juice on oral pharmacokinetics of riluzole in Wistar rats. The Journal of pharmacy and pharmacology. 2013 Mar; 65(3):337-44. doi: 10.1111/j.2042-7158.2012.01604.x. [PMID: 23356842]
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