Tegaserod (BioDeep_00000406032)
代谢物信息卡片
Tegaserod
化学式: C16H23N5O (301.1902508)
中文名称: 替加色罗
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CCCCCN=C(N)NN=CC1=CNC2=C1C=C(C=C2)OC
InChI: InChI=1S/C16H23N5O/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21)/b20-11+
描述信息
D018377 - Neurotransmitter Agents > D018490 - Serotonin Agents > D017366 - Serotonin Receptor Agonists
A - Alimentary tract and metabolism > A06 - Drugs for constipation > A06A - Drugs for constipation
C78272 - Agent Affecting Nervous System > C66885 - Serotonin Antagonist
Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research[1][2][3].
同义名列表
1 个代谢物同义名
数据库引用编号
14 个数据库交叉引用编号
- ChEBI: CHEBI:51043
- ChEBI: CHEBI:94540
- KEGGdrug: D06056
- PubChem: 135409453
- Metlin: METLIN44186
- DrugBank: DB01079
- ChEMBL: CHEMBL76370
- CAS: 1044642-88-7
- CAS: 145158-71-0
- MoNA: FiehnHILIC003005
- MoNA: FiehnHILIC002348
- MoNA: FiehnHILIC000781
- RefMet: Tegaserod
- medchemexpress: HY-14153
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。
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文献列表
- Paul A Gurbel, Kevin Bliden, Scott D Barnett, Casey Witt, Heng Zou, Udaya Tantry. An Ex Vivo Study to Evaluate the Effect of Tegaserod on Platelet Activation and Aggregation.
Journal of cardiovascular pharmacology and therapeutics.
2021 01; 26(1):40-50. doi:
10.1177/1074248420942004. [PMID: 32672062] - Motoshi Okumura, Akihiro Hamada, Fumina Ohsaka, Takeshi Tsuruta, Tohru Hira, Kei Sonoyama. Expression of serotonin receptor HTR4 in glucagon-like peptide-1-positive enteroendocrine cells of the murine intestine.
Pflugers Archiv : European journal of physiology.
2020 10; 472(10):1521-1532. doi:
10.1007/s00424-020-02453-7. [PMID: 32870377] - Deborah L Higgins, Mike P Ero, Michelle Loeb, Kathryn Kersey, Alan Hopkins, David T Beattie. The inability of tegaserod to affect platelet aggregation and coronary artery tone at supratherapeutic concentrations.
Naunyn-Schmiedeberg's archives of pharmacology.
2012 Jan; 385(1):103-9. doi:
10.1007/s00210-011-0687-x. [PMID: 21901313] - Victor L Serebruany, Mohamed El Mouelhi, Hans-Jürgen Pfannkuche, Kristine Rose, Martin Marro, Dominick J Angiolillo. Investigations on 5-HT₄ receptor expression and effects of tegaserod on human platelet aggregation in vitro.
American journal of therapeutics.
2010 Nov; 17(6):543-52. doi:
10.1097/mjt.0b013e3181b63f21. [PMID: 19797939] - Christopher Keating, Vicente Martinez, Lorna Ewart, Stephen Gibbons, Luke Grundy, Jean-Pierre Valentin, David Grundy. The validation of an in vitro colonic motility assay as a biomarker for gastrointestinal adverse drug reactions.
Toxicology and applied pharmacology.
2010 Jun; 245(3):299-309. doi:
10.1016/j.taap.2010.03.014. [PMID: 20350559] - 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] - Ramakrishna Nirogi, Vishwottam Kandikere, Koteshwara Mudigonda. Sensitive liquid chromatography positive electrospray tandem mass spectrometry method for the quantitation of tegaserod in human plasma using liquid-liquid extraction.
Journal of chromatographic science.
2009 Feb; 47(2):164-9. doi:
10.1093/chromsci/47.2.164. [PMID: 19222925] - Ryosuke Kojima, Hitoshi Doihara, Katsura Nozawa, Eri Kawabata-Shoda, Toshihide Yokoyama, Hiroyuki Ito. Characterization of two models of drug-induced constipation in mice and evaluation of mustard oil in these models.
Pharmacology.
2009; 84(4):227-33. doi:
10.1159/000236524. [PMID: 19752586] - 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] - J A M Smith, D T Beattie, D Marquess, J P Shaw, R G Vickery, P P A Humphrey. The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity.
Naunyn-Schmiedeberg's archives of pharmacology.
2008 Jul; 378(1):125-37. doi:
10.1007/s00210-008-0282-y. [PMID: 18415081] - Shuang-Qing Zhang, Sridhar Thumma, Guo-Hua Chen, Wei-Bin Deng, Michael A Repka, San-Ming Li. In vitro and in vivo evaluation of tegaserod maleate pH-dependent tablets.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.
2008 May; 69(1):247-54. doi:
10.1016/j.ejpb.2007.10.010. [PMID: 18037278] - Jian-Jun Zou, Xiao-Jie Bian, Li Ding, Yu-Bin Zhu, Hong-Wei Fan, Da-Wei Xiao. Determination of tegaserod by LC-ESI-MS/MS and its application to a pharmacokinetic study in healthy Chinese volunteers.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2008 Jan; 861(1):151-7. doi:
10.1016/j.jchromb.2007.11.011. [PMID: 18069077] - M Thumshirn, H Fruehauf, B Stutz, G Tougas, J Salter, M Fried. Clinical trial: effects of tegaserod on gastric motor and sensory function in patients with functional dyspepsia.
Alimentary pharmacology & therapeutics.
2007 Nov; 26(10):1399-407. doi:
10.1111/j.1365-2036.2007.03521.x. [PMID: 17892526] - Yuyuan Li, Yuqiang Nie, Jun Xie, Weizhan Tang, Peizhi Liang, Weihong Sha, Hui Yang, Yonyjian Zhou. The association of serotonin transporter genetic polymorphisms and irritable bowel syndrome and its influence on tegaserod treatment in Chinese patients.
Digestive diseases and sciences.
2007 Nov; 52(11):2942-9. doi:
10.1007/s10620-006-9679-y. [PMID: 17394071] - M Camilleri. Pharmacogenomics and serotonergic agents: research observations and potential clinical practice implications.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society.
2007 Aug; 19 Suppl 2(?):40-5. doi:
10.1111/j.1365-2982.2007.00961.x. [PMID: 17620087] - Emmanuel Coron, Jan G Hatlebakk, Jean-Paul Galmiche. Medical therapy of gastroesophageal reflux disease.
Current opinion in gastroenterology.
2007 Jul; 23(4):434-9. doi:
10.1097/mog.0b013e328159f001. [PMID: 17545782] - Zhao-Lu Ding, Mei-Yun Ke, Xiao-Hong Sun, Zhi-Feng Wang. [Effect of combined drug treatment on megacolon with severe constipation].
Zhonghua yi xue za zhi.
2007 Mar; 87(10):670-2. doi:
". [PMID: 17553303] - Manfred G Ismair, Gerd A Kullak-Ublick, Randy D Blakely, Michael Fried, Stephan R Vavricka. Tegaserod inhibits the serotonin transporter SERT.
Digestion.
2007; 75(2-3):90-5. doi:
10.1159/000102962. [PMID: 17510552] - Michelle L Delco, Jorge E Nieto, Arthur L Craigmill, Scott D Stanley, Jack R Snyder. Pharmacokinetics and in vitro effects of tegaserod, a serotonin 5-hydroxytryptamine 4 (5-HT4) receptor agonist with prokinetic activity in horses.
Veterinary therapeutics : research in applied veterinary medicine.
2007; 8(1):77-87. doi:
NULL. [PMID: 17447227] - Erik Hedner, Martin Sjögren, Per-Anders Frändberg, Tobias Johansson, Ulf Göransson, Mia Dahlström, Per Jonsson, Fred Nyberg, Lars Bohlin. Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
Journal of natural products.
2006 Oct; 69(10):1421-4. doi:
10.1021/np0601760. [PMID: 17067154] - Derek J Roberts, Hoan Linh Banh, Richard I Hall. Use of novel prokinetic agents to facilitate return of gastrointestinal motility in adult critically ill patients.
Current opinion in critical care.
2006 Aug; 12(4):295-302. doi:
10.1097/01.ccx.0000235205.54579.5d. [PMID: 16810038] - Yu-yuan Li, Yu-qiang Nie, Jun Xie, Hui-zhen Tan, Yong-jian Zhou, Hong Wang. [Serotonin transporter gene polymorphisms in irritable bowel syndrome and their impact on tegaserod treatment].
Zhonghua nei ke za zhi.
2006 Jul; 45(7):552-5. doi:
NULL. [PMID: 17074108] - Ronald Mathison, Eldon Shaffer, Hans-Juergen Pfannkuche, David Earnest. Effects of tegaserod on bile composition and hepatic secretion in Richardson ground squirrels on an enriched cholesterol diet.
Lipids in health and disease.
2006 Jun; 5(?):15. doi:
10.1186/1476-511x-5-15. [PMID: 16792807] - Ronald Mathison, Eldon Shaffer. Increased cholinergic contractions of jejunal smooth muscle caused by a high cholesterol diet are prevented by the 5-HT4 agonist--tegaserod.
BMC gastroenterology.
2006 Feb; 6(?):8. doi:
10.1186/1471-230x-6-8. [PMID: 16504074] - J J Galligan, S Vanner. Basic and clinical pharmacology of new motility promoting agents.
Neurogastroenterology and motility.
2005 Oct; 17(5):643-53. doi:
10.1111/j.1365-2982.2005.00675.x. [PMID: 16185302] - B S Lippold, J Hildebrand, R Straub. Tegaserod (HTF 919) stimulates gut motility in normal horses.
Equine veterinary journal.
2004 Nov; 36(7):622-7. doi:
10.2746/0425164044864543. [PMID: 15581328] - D T Beattie, J A M Smith, D Marquess, R G Vickery, S R Armstrong, T Pulido-Rios, J L McCullough, C Sandlund, C Richardson, N Mai, P P A Humphrey. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
British journal of pharmacology.
2004 Nov; 143(5):549-60. doi:
10.1038/sj.bjp.0705929. [PMID: 15466450] - Robert S Fisher, Johnson Thistle, Anthony Lembo, James Novick, Patrick O'Kane, William D Chey, Christoph Beglinger, Peter Rueegg, Victor Shi, Angeli Dogra, Dongham Luo, David L Earnest. Tegaserod does not alter fasting or meal-induced biliary tract motility.
The American journal of gastroenterology.
2004 Jul; 99(7):1342-9. doi:
10.1111/j.1572-0241.2004.30301.x. [PMID: 15233676] - William L Hasler, Philip Schoenfeld. Safety profile of tegaserod, a 5-HT4 receptor agonist, for the treatment of irritable bowel syndrome.
Drug safety.
2004; 27(9):619-31. doi:
10.2165/00002018-200427090-00001. [PMID: 15230644] - Suzanne K Swan, Honghui Zhou, Ann Horowitz, Latifa Alladina, Martine Hubert, Silke Appel-Dingemanse, Stuart Osborne, Larry Lambrecht, James F McLeod. Tegaserod pharmacokinetics are similar in patients with severe renal insufficiency and in healthy subjects.
Journal of clinical pharmacology.
2003 Apr; 43(4):359-64. doi:
10.1177/0091270003251823. [PMID: 12723456] - Joel Morganroth, Peter C Rüegg, Cornelia Dunger-Baldauf, Silke Appel-Dingemanse, Harald Bliesath, Martin Lefkowitz. Tegaserod, a 5-hydroxytryptamine type 4 receptor partial agonist, is devoid of electrocardiographic effects.
The American journal of gastroenterology.
2002 Sep; 97(9):2321-7. doi:
10.1111/j.1572-0241.2002.05986.x. [PMID: 12358251] - Silke Appel-Dingemanse. Clinical pharmacokinetics of tegaserod, a serotonin 5-HT(4) receptor partial agonist with promotile activity.
Clinical pharmacokinetics.
2002; 41(13):1021-42. doi:
10.2165/00003088-200241130-00002. [PMID: 12403641] - H Zhou, A Horowitz, P C Ledford, M Hubert, S Appel-Dingemanse, S Osborne, J F McLeod. The effects of tegaserod (HTF 919) on the pharmacokinetics and pharmacodynamics of digoxin in healthy subjects.
Journal of clinical pharmacology.
2001 Oct; 41(10):1131-9. doi:
10.1177/00912700122012625. [PMID: 11583482] - A E Vickers, M Zollinger, R Dannecker, R Tynes, F Heitz, V Fischer. In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions.
Drug metabolism and disposition: the biological fate of chemicals.
2001 Oct; 29(10):1269-76. doi:
NULL. [PMID: 11560869] - S Appel-Dingemanse, Y Hirschberg, S Osborne, F Pommier, J McLeod. Multiple-dose pharmacokinetics confirm no accumulation and dose proportionality of the novel promotile drug tegaserod (HTF 919).
European journal of clinical pharmacology.
2001 Mar; 56(12):889-91. doi:
10.1007/s002280000239. [PMID: 11317476] - H Zhou, S Khalilieh, H Lau, M Guerret, S Osborne, L Alladina, A L Laurent, J F McLeod. Effect of meal timing not critical for the pharmacokinetics of tegaserod (HTF 919).
Journal of clinical pharmacology.
1999 Sep; 39(9):911-9. doi:
10.1177/00912709922008524. [PMID: 10471981] - M D Drici, S N Ebert, W X Wang, I Rodriguez, X K Liu, B H Whitfield, R L Woosley. Comparison of tegaserod (HTF 919) and its main human metabolite with cisapride and erythromycin on cardiac repolarization in the isolated rabbit heart.
Journal of cardiovascular pharmacology.
1999 Jul; 34(1):82-8. doi:
10.1097/00005344-199907000-00014. [PMID: 10413072]