Ibudilast (BioDeep_00000033353)

   

human metabolite blood metabolite


代谢物信息卡片


2-methyl-1-[2-(propan-2-yl)pyrazolo[1,5-a]pyridin-3-yl]propan-1-one

化学式: C14H18N2O (230.1419058)
中文名称: 异丁司特
谱图信息: 最多检出来源 Homo sapiens(blood) 8.73%

分子结构信息

SMILES: CC(C)C(=O)C1=C2C=CC=CN2N=C1C(C)C
InChI: InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3

描述信息

Ibudilast is an anti-inflammatory and neuroprotective oral agent which shows an excellent safety profile at 60 mg/day and provides significantly prolonged time-to-first relapse and attenuated brain volume shrinkage in patients with relapsing-remitting (RR) and/or secondary progressive (SP) multiple sclerosis (MS). Ibudilast is currently in development in the U.S. (codes: AV-411 or MN-166), but is approved for use as an antiinflammatory in Japan.
R - Respiratory system > R03 - Drugs for obstructive airway diseases > R03D - Other systemic drugs for obstructive airway diseases > R03DC - Leukotriene receptor antagonists
D019141 - Respiratory System Agents > D018927 - Anti-Asthmatic Agents > D001993 - Bronchodilator Agents
COVID info from clinicaltrial, clinicaltrials, clinical trial, clinical trials
C78274 - Agent Affecting Cardiovascular System > C29707 - Vasodilating Agent
C78275 - Agent Affecting Blood or Body Fluid > C1327 - Antiplatelet Agent
D006401 - Hematologic Agents > D010975 - Platelet Aggregation Inhibitors
D018373 - Peripheral Nervous System Agents > D001337 - Autonomic Agents
D004791 - Enzyme Inhibitors > D010726 - Phosphodiesterase Inhibitors
D002317 - Cardiovascular Agents > D014665 - Vasodilator Agents
Corona-virus
Coronavirus
SARS-CoV-2
COVID-19
SARS-CoV
COVID19
SARS2
SARS

同义名列表

16 个代谢物同义名

2-methyl-1-[2-(propan-2-yl)pyrazolo[1,5-a]pyridin-3-yl]propan-1-one; 3-Isobutyryl-2-isopropyl-pyrazolo(1,5-a)pyridine; 3-Isobutyryl-2-isopropylpyrazolo(1,5-a)pyridine; 3-Isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine; 2-Isopropyl-3-isobutyrylpyrazolo(1,5-a)pyridine; UNII-m0TTH61XC5; Lopac-I-0157; Ibudilastum; I0157_sigma; Tocris-1694; Ibudilast; Eyevinal; MN-166; Ke tas; AV-411; Ketas



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

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

  • Erica N Grodin, Steven J Nieto, Lindsay R Meredith, Elizabeth Burnette, Joseph O'Neill, Jeffry Alger, Edythe D London, Karen Miotto, Christopher J Evans, Michael R Irwin, Lara A Ray. Effects of ibudilast on central and peripheral markers of inflammation in alcohol use disorder: A randomized clinical trial. Addiction biology. 2022 07; 27(4):e13182. doi: 10.1111/adb.13182. [PMID: 35754106]
  • Robert J Fox, Paola Raska, Christian Barro, Matthew Karafa, Victoria Konig, Robert A Bermel, Marianne Chase, Christopher S Coffey, Andrew D Goodman, Eric C Klawiter, Robert T Naismith, Jens Kuhle. Neurofilament light chain in a phase 2 clinical trial of ibudilast in progressive multiple sclerosis. Multiple sclerosis (Houndmills, Basingstoke, England). 2021 11; 27(13):2014-2022. doi: 10.1177/1352458520986956. [PMID: 33635141]
  • Nobuaki Egashira, Yu Goto, Ryota Takahashi, Hikari Iba, Shota Yamamoto, Takuya Watanabe, Kaori Kubota, Takehiro Kawashiri, Chise Taniguchi, Shutaro Katsurabayashi, Katsunori Iwasaki. Ibudilast suppresses oxaliplatin-induced mechanical allodynia and neurodegeneration in rats. Journal of pharmacological sciences. 2021 Sep; 147(1):114-117. doi: 10.1016/j.jphs.2021.06.004. [PMID: 34294361]
  • 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]
  • Shouma Ishikawa, Atsushi Sawamoto, Satoshi Okuyama, Mitsunari Nakajima. T-Cell Activation-Inhibitory Assay to Screen Caloric Restriction Mimetics Drugs for Drug Repositioning. Biological & pharmaceutical bulletin. 2021; 44(4):550-556. doi: 10.1248/bpb.b20-00889. [PMID: 33790105]
  • Suma Babu, Baileigh G Hightower, James Chan, Nicole R Zürcher, Pia Kivisäkk, Chieh-En J Tseng, Danica L Sanders, Ashley Robichaud, Haruhiko Banno, Armineuza Evora, Akshata Ashokkumar, Lindsay Pothier, Sabrina Paganoni, Sheena Chew, Joanna Dojillo, Kazuko Matsuda, Mark Gudesblatt, James D Berry, Merit E Cudkowicz, Jacob M Hooker, Nazem Atassi. Ibudilast (MN-166) in amyotrophic lateral sclerosis- an open label, safety and pharmacodynamic trial. NeuroImage. Clinical. 2021; 30(?):102672. doi: 10.1016/j.nicl.2021.102672. [PMID: 34016561]
  • Elizabeth M Burnette, Wave-Ananda Baskerville, Erica N Grodin, Lara A Ray. Ibudilast for alcohol use disorder: study protocol for a phase II randomized clinical trial. Trials. 2020 Sep; 21(1):779. doi: 10.1186/s13063-020-04670-y. [PMID: 32912290]
  • Lien D Nguyen, Tom T Fischer, Damien Abreu, Alfredo Arroyo, Fumihiko Urano, Barbara E Ehrlich. Calpain inhibitor and ibudilast rescue β cell functions in a cellular model of Wolfram syndrome. Proceedings of the National Academy of Sciences of the United States of America. 2020 07; 117(29):17389-17398. doi: 10.1073/pnas.2007136117. [PMID: 32632005]
  • Nan-Chun Wu, Jiun-Jr Wang. Ibudilast, a Phosphodiesterase Inhibitor and Toll-Like Receptor-4 Antagonist, Improves Hemorrhagic Shock and Reperfusion-Induced Left Ventricular Dysfunction by Reducing Myocardial Tumor Necrosis Factor α. Transplantation proceedings. 2020 Jul; 52(6):1869-1874. doi: 10.1016/j.transproceed.2020.02.145. [PMID: 32631581]
  • Keith G Heinzerling, Marisa Briones, April D Thames, Charles H Hinkin, Tianle Zhu, Ying Nian Wu, Steven J Shoptaw. Randomized, Placebo-Controlled Trial of Targeting Neuroinflammation with Ibudilast to Treat Methamphetamine Use Disorder. Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology. 2020 06; 15(2):238-248. doi: 10.1007/s11481-019-09883-w. [PMID: 31820289]
  • Dongjie Yang, Yihan Yang, Yue Zhao. Ibudilast, a Phosphodiesterase-4 Inhibitor, Ameliorates Acute Respiratory Distress Syndrome in Neonatal Mice by Alleviating Inflammation and Apoptosis. Medical science monitor : international medical journal of experimental and clinical research. 2020 Mar; 26(?):e922281. doi: 10.12659/msm.922281. [PMID: 32231178]
  • 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]
  • B Łebkowska-Wieruszewska, V De Vito, C J Kowalski, H Owen, A Poapolathep, A Lisowski, M Giorgi. Pharmacokinetic profiles of 5 mg/kg ibudilast, a phosphodiesterase inhibitor, orally administered to dogs in fasted and non-fasted states. A preliminary study. Polish journal of veterinary sciences. 2018 Jun; 21(2):281-285. doi: 10.24425/119049. [PMID: 30450866]
  • Ernesto Roque Bongarzone, Maria Luisa Escolar, Steven James Gray, Tal Kafri, Charles Herman Vite, Mark Steven Sands. Insights into the Pathogenesis and Treatment of Krabbe Disease. Pediatric endocrinology reviews : PER. 2016 Jun; 13 Suppl 1(?):689-96. doi: . [PMID: 27491217]
  • Erica Zamberletti, Marina Gabaglio, Pamela Prini, Tiziana Rubino, Daniela Parolaro. Cortical neuroinflammation contributes to long-term cognitive dysfunctions following adolescent delta-9-tetrahydrocannabinol treatment in female rats. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2015 Dec; 25(12):2404-15. doi: 10.1016/j.euroneuro.2015.09.021. [PMID: 26499171]
  • Hwa Yoon, Hea-Young Cho, Yong-Bok Lee. Determination of ibudilast in human serum by high-performance liquid chromatography for pharmacokinetic study. Biomedical chromatography : BMC. 2010 Mar; 24(3):324-8. doi: 10.1002/bmc.1293. [PMID: 19629961]
  • L M Sanftner, J A Gibbons, M I Gross, B M Suzuki, F C A Gaeta, K W Johnson. Cross-species comparisons of the pharmacokinetics of ibudilast. Xenobiotica; the fate of foreign compounds in biological systems. 2009 Dec; 39(12):964-77. doi: 10.3109/00498250903254340. [PMID: 19925385]
  • Mark R Hutchinson, Susannah S Lewis, Benjamen D Coats, David A Skyba, Nicole Y Crysdale, Debra L Berkelhammer, Anita Brzeski, Alexis Northcutt, Christine M Vietz, Charles M Judd, Steven F Maier, Linda R Watkins, Kirk W Johnson. Reduction of opioid withdrawal and potentiation of acute opioid analgesia by systemic AV411 (ibudilast). Brain, behavior, and immunity. 2009 Feb; 23(2):240-50. doi: 10.1016/j.bbi.2008.09.012. [PMID: 18938237]
  • Paul Rolan, Jacqueline A Gibbons, Lin He, Eppie Chang, Drew Jones, Matthew I Gross, Jennifer Bahr Davidson, Laura M Sanftner, Kirk W Johnson. Ibudilast in healthy volunteers: safety, tolerability and pharmacokinetics with single and multiple doses. British journal of clinical pharmacology. 2008 Dec; 66(6):792-801. doi: 10.1111/j.1365-2125.2008.03270.x. [PMID: 19032723]
  • Tongling Li, Yinuo Pang, Zhixiao Wang, Yurong Jia, Qiang Cheng, Jian Sun. [Pharmacokinetics and relative bioavailability of KC-404 sustained release tablets in healthy volunteers]. Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition. 2003 Jul; 34(3):541-3. doi: NULL. [PMID: 12910715]
  • G Rile, Y Yatomi, R Qi, K Satoh, Y Ozaki. Potentiation of ibudilast inhibition of platelet aggregation in the presence of endothelial cells. Thrombosis research. 2001 May; 102(3):239-46. doi: 10.1016/s0049-3848(01)00258-4. [PMID: 11369417]
  • A Suzumura, A Ito, M Yoshikawa, M Sawada. Ibudilast suppresses TNFalpha production by glial cells functioning mainly as type III phosphodiesterase inhibitor in the CNS. Brain research. 1999 Aug; 837(1-2):203-12. doi: 10.1016/s0006-8993(99)01666-2. [PMID: 10434004]
  • M Ichinose, K Kimura, T Takahashi, M Miura, H Inoue, T Takishima, K Shirato. Antiasthma drug, ibudilast, inhibits neurogenic plasma extravasation in guinea-pig airways. The American review of respiratory disease. 1993 Aug; 148(2):431-4. doi: 10.1164/ajrccm/148.2.431. [PMID: 8342908]
  • H Onodera, M Okamoto, S Takemura, T Doi, Y Kasamatsu, K Yanagida, W Fukuda, M Tanaka, M Deguchi, M Ueda. [Complement fragments in patients with bronchial asthma]. Arerugi = [Allergy]. 1991 Oct; 40(10):1272-81. doi: NULL. [PMID: 1772350]
  • M Yasui, K Ota, A Oshima. Effects of ibudilast on calcium deposition in soft tissues of rabbits with atherosclerosis. The Journal of international medical research. 1990 Sep; 18(5):415-24. doi: 10.1177/030006059001800510. [PMID: 2257963]