Tropisetron hydrochloride (BioDeep_00000839710)
代谢物信息卡片
Tropisetron hydrochloride
化学式: C17H21ClN2O2 (320.1291476)
中文名称: 盐酸托烷司琼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43.Cl
InChI: 1H/t11-,12+,13?
描述信息
C78272 - Agent Affecting Nervous System > C66885 - Serotonin Antagonist > C94726 - 5-HT3 Receptor Antagonist
D018377 - Neurotransmitter Agents > D018490 - Serotonin Agents > D012702 - Serotonin Antagonists
D018373 - Peripheral Nervous System Agents > D001337 - Autonomic Agents
C78272 - Agent Affecting Nervous System > C267 - Antiemetic Agent
D005765 - Gastrointestinal Agents > D000932 - Antiemetics
D002491 - Central Nervous System Agents
Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. IC50 value: 70.1 ± 0.9 nM Target: 5-HT3 receptor; α7-nicotinic receptor in vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105\% compared to controls. Inhibition studies using the alpha7 nAChR antagonist, MLA (10 nM), support the hypothesis that tropisetron is an effective neuroprotective agent against glutamate-induced excitotoxicity; mediated by α7 nAChR activation. Tropisetron had no discernible effects on pAkt levels but significantly decreased p38 MAPK levels associated with excitotoxicity from an average of 15 ng/ml to 6 ng/ml [2]. Tropisetron, but not granisetron, significantly inhibits the phosphatase activity of calcineurin, over-expresses the CB(1) receptors at both transcriptional and protein levels, and reduces cAMP content in cerebellar granule neurons (CGNs) [4]. in vivo: Animals were treated intracerebroventricularly with tropisetron, mCPBG (selective 5-HT3 receptor agonist) or mCPBG plus tropisetron on days 1, 3, 5 and 7. Tropisetron significantly diminished the elevated levels of these markers and reversed the cognitive deficit. Interestingly, tropisetron was also found to be a potent inhibitor of calcineurin phosphatase activity [1]. tropisetron (5mg/kg/day) plus mCPBG (10mg/kg/day), and granisetron (5mg/kg/day) intraperitoneally on days 3-35 post-immunization. Treatment with tropisetron and granisetron markedly suppressed the clinical symptoms of EAE (p<0.001) and reduced leukocyte infiltration as well as demyelination in the spinal cord (p<0.05) [3].
同义名列表
数据库引用编号
9 个数据库交叉引用编号
- ChEBI: CHEBI:77570
- KEGGdrug: D02041
- PubChem: 656664
- ChEMBL: CHEMBL2130744
- ChEMBL: CHEMBL4303202
- MeSH: Tropisetron
- CAS: 105826-92-4
- CAS: 89613-86-5
- medchemexpress: HY-B0020
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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BioCyc(0)
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COVID-19 Disease Map(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
- Dongbin Zhang, ShangKun Si, WeiXun Shang, Xi Zhou. Effect of preoperative tropisetron treatment on postoperative cognitive function: A retrospective cohort study.
Medicine.
2022 Dec; 101(52):e32562. doi:
10.1097/md.0000000000032562. [PMID: 36596014] - Shiva Gholizadeh-Ghaleh Aziz, Roya Naderi, Nima Mahmodian. Ameliorative effects of tropisetron on liver injury in streptozotocin-induced diabetic rats.
Archives of physiology and biochemistry.
2021 Aug; 127(4):367-372. doi:
10.1080/13813455.2019.1640743. [PMID: 31306054] - Qiuju Xiong, Su Min, Ke Wei, Yanmei Yang, Jingyue Ma, Dan Liu, Menghua Zeng, Lei Zou. Transcutaneous Electrical Acupoint Stimulation Combined with Dexamethasone and Tropisetron Prevents Postoperative Nausea and Vomiting in Female Patients Undergoing Laparoscopic Sleeve Gastrectomy: a Prospective, Randomized Controlled Trial.
Obesity surgery.
2021 05; 31(5):1912-1920. doi:
10.1007/s11695-020-05205-9. [PMID: 33650089] - Bagher Pourheydar, Mahrokh Samadi, Parisa Habibi, Ahmad Ali Nikibakhsh, Roya Naderi. Renoprotective effects of tropisetron through regulation of the TGF-β1, p53 and matrix metalloproteinases in streptozotocin-induced diabetic rats.
Chemico-biological interactions.
2021 Feb; 335(?):109332. doi:
10.1016/j.cbi.2020.109332. [PMID: 33387473] - Mahrokh Samadi, Shiva Gholizadeh-Ghaleh Aziz, Roya Naderi. The effect of tropisetron on oxidative stress, SIRT1, FOXO3a, and claudin-1 in the renal tissue of STZ-induced diabetic rats.
Cell stress & chaperones.
2021 01; 26(1):217-227. doi:
10.1007/s12192-020-01170-5. [PMID: 33047279] - Roya Naderi, Alireza Shirpoor, Mahrokh Samadi, Bagher Pourheydar, Azam Moslehi. Tropisetron attenuates pancreas apoptosis in the STZ-induced diabetic rats: involvement of SIRT1/NF-κB signaling.
Pharmacological reports : PR.
2020 Dec; 72(6):1657-1665. doi:
10.1007/s43440-020-00146-7. [PMID: 32725585] - Ashkan Divanbeigi, Mohammad Nasehi, Salar Vaseghi, Sepideh Amiri, Mohammad-Reza Zarrindast. Tropisetron But Not Granisetron Ameliorates Spatial Memory Impairment Induced by Chronic Cerebral Hypoperfusion.
Neurochemical research.
2020 Nov; 45(11):2631-2640. doi:
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European journal of pharmacology.
2020 Sep; 883(?):173310. doi:
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The Journal of pharmacy and pharmacology.
2020 Aug; 72(8):1082-1091. doi:
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Hormone molecular biology and clinical investigation.
2020 May; 41(3):. doi:
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European journal of pharmacology.
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Clinical and experimental pharmacology & physiology.
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European journal of pharmacology.
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Neurotoxicology.
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Minerva anestesiologica.
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Cardiovascular toxicology.
2012 Dec; 12(4):318-25. doi:
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The pharmacogenomics journal.
2012 Feb; 12(1):22-9. doi:
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PloS one.
2012; 7(12):e53203. doi:
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International immunopharmacology.
2011 Dec; 11(12):2073-8. doi:
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Pain.
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European journal of clinical investigation.
2009 May; 39(5):375-83. doi:
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Journal of pharmaceutical and biomedical analysis.
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Scandinavian journal of rheumatology. Supplement.
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Scandinavian journal of rheumatology. Supplement.
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