Triazolam (BioDeep_00000017986)

   

human metabolite blood metabolite Chemicals and Drugs


代谢物信息卡片


12-chloro-9-(2-chlorophenyl)-3-methyl-2,4,5,8-tetraazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaene

化学式: C17H12Cl2N4 (342.0438972)
中文名称: 三唑仑
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CC1=NN=C2CN=C(C3=CC=CC=C3Cl)C3=C(C=CC(Cl)=C3)N12
InChI: InChI=1S/C17H12Cl2N4/c1-10-21-22-16-9-20-17(12-4-2-3-5-14(12)19)13-8-11(18)6-7-15(13)23(10)16/h2-8H,9H2,1H3

描述信息

Triazolam is only found in individuals that have used or taken this drug.It is withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
N - Nervous system > N05 - Psycholeptics > N05C - Hypnotics and sedatives > N05CD - Benzodiazepine derivatives
D002492 - Central Nervous System Depressants > D014149 - Tranquilizing Agents > D014151 - Anti-Anxiety Agents
D002491 - Central Nervous System Agents > D011619 - Psychotropic Drugs > D014149 - Tranquilizing Agents
C78272 - Agent Affecting Nervous System > C29756 - Sedative and Hypnotic > C1012 - Benzodiazepine
D002491 - Central Nervous System Agents > D002492 - Central Nervous System Depressants
D018377 - Neurotransmitter Agents > D018682 - GABA Agents > D018757 - GABA Modulators
C78272 - Agent Affecting Nervous System > C28197 - Antianxiety Agent

同义名列表

14 个代谢物同义名

12-chloro-9-(2-chlorophenyl)-3-methyl-2,4,5,8-tetraazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaene; Genpharm brand OF triazolam; Apotex brand OF triazolam; Pfizer brand OF triazolam; Gerard brand OF triazolam; Triazolam pfizer brand; Gen triazolam; Gen-triazolam; DEA no. 2887; Apo-triazo; Apo triazo; triazolam; Halcion; Trilam



数据库引用编号

10 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

  • QingLiang Wu, YiTing Hu, CuiTong Wang, Wei Wei, LanLan Gui, WuShuang Zeng, Changxiao Liu, Wei Jia, Jia Miao, Ke Lan. Reevaluate In Vitro CYP3A Index Reactions of Benzodiazepines and Steroids between Humans and Dogs. Drug metabolism and disposition: the biological fate of chemicals. 2022 06; 50(6):741-749. doi: 10.1124/dmd.122.000864. [PMID: 35351776]
  • Hiroshi Arakawa, Shinji Sugiura, Takumi Kawanishi, Kazumi Shin, Hiroko Toyoda, Taku Satoh, Yasuyuki Sakai, Toshiyuki Kanamori, Yukio Kato. Kinetic analysis of sequential metabolism of triazolam and its extrapolation to humans using an entero-hepatic two-organ microphysiological system. Lab on a chip. 2020 02; 20(3):537-547. doi: 10.1039/c9lc00884e. [PMID: 31930237]
  • Shinji Iwasaki, Yohei Kosugi, Andy Z X Zhu, Sayaka Nakagawa, Noriyasu Sano, Miyuki Funami, Mai Kosaka, Atsutoshi Furuta, Hideki Hirabayashi, Nobuyuki Amano. Application of unbound liver-to-plasma concentration ratio to quantitative projection of cytochrome P450-mediated drug-drug interactions using physiologically based pharmacokinetic modelling approach. Xenobiotica; the fate of foreign compounds in biological systems. 2019 Nov; 49(11):1251-1259. doi: 10.1080/00498254.2018.1547461. [PMID: 30516093]
  • 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]
  • Genki Minegishi, Yasuhiro Kazuki, Yuki Yamasaki, Fuka Okuya, Hidetaka Akita, Mitsuo Oshimura, Kaoru Kobayashi. Comparison of the hepatic metabolism of triazolam in wild-type andCyp3a-knockout mice for understanding CYP3A-mediated metabolism inCYP3A-humanised mice in vivo. Xenobiotica; the fate of foreign compounds in biological systems. 2019 Nov; 49(11):1303-1310. doi: 10.1080/00498254.2018.1560516. [PMID: 30561249]
  • Shweta Padmanabhan, Harbeer Kaur, Abhijith Rao, Ajay Saxena, Yogesh Kumar Gupta, T Thanga Mariappan, Vinay K Holenarsipur. Effect of pretreatment regimens of 1-aminobenzotriazole on metabolism and gastric emptying of probe compounds in rat. Xenobiotica; the fate of foreign compounds in biological systems. 2019 Jun; 49(6):646-654. doi: 10.1080/00498254.2018.1489166. [PMID: 29898636]
  • Harunobu Tahara, Miwa Watanabe, Maki Hasegawa. A comparative study for detecting CYP3A induction by CYP3A probe drugs and endogenous markers in cynomolgus monkeys. Biopharmaceutics & drug disposition. 2019 Feb; 40(2):81-93. doi: 10.1002/bdd.2173. [PMID: 30724384]
  • Yohei Koya, Shinya Uchida, Yoshiki Machi, Yuko Shobu, Noriyuki Namiki, Tsutomu Kotegawa. Prediction of drug interaction between oral adsorbent AST-120 and concomitant drugs based on the in vitro dissolution and in vivo absorption behavior of the drugs. European journal of clinical pharmacology. 2016 Nov; 72(11):1353-1361. doi: 10.1007/s00228-016-2102-5. [PMID: 27491774]
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  • Kimiko Tsutsumi, Miyuki Iwao, Tsutomu Kotegawa, Hiromitsu Imai, Kyoichi Ohashi, Shigeyuki Nakano. [Determination of triazolam and midazolam in human plasma using gas chromatography with microelectron capture detection for clinical application]. Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan. 2014; 134(1):119-25. doi: 10.1248/yakushi.13-00153. [PMID: 24389624]
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  • Akira Namera, Ryosuke Makita, Tatsuro Saruwatari, Aiko Hatano, Hiroaki Shiraishi, Masataka Nagao. Acute intoxication caused by overdose of flunitrazepam and triazolam: high concentration of metabolites detected at autopsy examination. The American journal of forensic medicine and pathology. 2012 Dec; 33(4):293-6. doi: 10.1097/paf.0b013e31820f1514. [PMID: 21372658]
  • Tsutomu Kotegawa, Kimiko Tsutsumi, Hajime Morita, Hiromistu Imai, Misaki Morita, Tsuneaki Yoshizato, Tetsuji Ohyama, Shinya Uchida, Hiroshi Watanabe, Noriyuki Namiki, Kyoichi Ohashi. Effects of dosing interval on the pharmacokinetic and pharmacodynamic interactions between the oral adsorbent AST-120 and triazolam in humans. European journal of clinical pharmacology. 2012 Dec; 68(12):1605-10. doi: 10.1007/s00228-012-1301-y. [PMID: 22644342]
  • Stephanie J Marin, Mark Roberts, Michelle Wood, Gwendolyn A McMillin. Sensitive UPLC-MS-MS assay for 21 benzodiazepine drugs and metabolites, zolpidem and zopiclone in serum or plasma. Journal of analytical toxicology. 2012 Sep; 36(7):472-6. doi: 10.1093/jat/bks059. [PMID: 22833647]
  • Masataka Tajima, Nobutomo Ikarashi, Yukari Imahori, Takehiro Okaniwa, Kanako Saruta, Makoto Ishii, Yoshiki Kusunoki, Risako Kon, Takahiro Toda, Wataru Ochiai, Harumi Yamada, Kiyoshi Sugiyama. Consumption of a high-fat diet during pregnancy decreases the activity of cytochrome P450 3a in the livers of offspring. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2012 Aug; 47(1):108-16. doi: 10.1016/j.ejps.2012.05.008. [PMID: 22659374]
  • Ruth Verplaetse, Eva Cuypers, Jan Tytgat. The evaluation of the applicability of a high pH mobile phase in ultrahigh performance liquid chromatography tandem mass spectrometry analysis of benzodiazepines and benzodiazepine-like hypnotics in urine and blood. Journal of chromatography. A. 2012 Aug; 1249(?):147-54. doi: 10.1016/j.chroma.2012.06.023. [PMID: 22749457]
  • S Stybe Johansen, R Dahl-Sørensen. A drug rape case involving triazolam detected in hair and urine. International journal of legal medicine. 2012 Jul; 126(4):637-43. doi: 10.1007/s00414-011-0654-6. [PMID: 22160334]
  • Pertti J Neuvonen. Towards safer and more predictable drug treatment--reflections from studies of the First BCPT Prize awardee. Basic & clinical pharmacology & toxicology. 2012 Mar; 110(3):207-18. doi: 10.1111/j.1742-7843.2012.00858.x. [PMID: 22348413]
  • Maki Hasegawa, Harunobu Tahara, Ryo Inoue, Masakazu Kakuni, Chise Tateno, Junko Ushiki. Investigation of drug-drug interactions caused by human pregnane X receptor-mediated induction of CYP3A4 and CYP2C subfamilies in chimeric mice with a humanized liver. Drug metabolism and disposition: the biological fate of chemicals. 2012 Mar; 40(3):474-80. doi: 10.1124/dmd.111.042754. [PMID: 22126990]
  • Kenji Kuwayama, Kenji Tsujikawa, Hajime Miyaguchi, Tatsuyuki Kanamori, Yuko T Iwata, Hiroyuki Inoue. Rapid, simple, and highly sensitive analysis of drugs in biological samples using thin-layer chromatography coupled with matrix-assisted laser desorption/ionization mass spectrometry. Analytical and bioanalytical chemistry. 2012 Jan; 402(3):1257-67. doi: 10.1007/s00216-011-5576-0. [PMID: 22147272]
  • Cyrus Ghobadi, Trevor N Johnson, Mohsen Aarabi, Lisa M Almond, Aurel Constant Allabi, Karen Rowland-Yeo, Masoud Jamei, Amin Rostami-Hodjegan. Application of a systems approach to the bottom-up assessment of pharmacokinetics in obese patients: expected variations in clearance. Clinical pharmacokinetics. 2011 Dec; 50(12):809-22. doi: 10.2165/11594420-000000000-00000. [PMID: 22087867]
  • Qing Chang, Hongying Ma, Fangjie Wang, Honglian Ou, Ming Zou. [Determination of 10 sedative-hypnotics in human plasma using pulse splitless injection technique and gas chromatography-mass spectrometry]. Se pu = Chinese journal of chromatography. 2011 Nov; 29(11):1082-6. doi: . [PMID: 22393695]
  • Shoetsu Chiba, Toru Ikawa, Hiroshi Takeshita, Kazue Ichiba, Morihisa Sagi, Toshiji Mukai, Naohiro Anzai. Interactions of human organic anion transporter 1 (hOAT1) with substances associated with forensic toxicology. Legal medicine (Tokyo, Japan). 2011 Jul; 13(4):180-5. doi: 10.1016/j.legalmed.2011.04.001. [PMID: 21561794]
  • Guoyou Jin, Baofei Zhang, Youwen Tang, Xiongjun Zuo, Songcai Wang, Jingyi Tang. Imprinted functionalized silica sol-gel for solid-phase extraction of triazolamin. Talanta. 2011 May; 84(3):644-50. doi: 10.1016/j.talanta.2011.01.035. [PMID: 21482262]
  • Akira Namera, Masakata Nagao, Akihiro Nakamoto, Shota Miyazaki, Takeshi Saito. Monolithic spin column: a new extraction device for analysis of drugs in urine and serum by GC/MS and HPLC/MS. Journal of AOAC International. 2011 May; 94(3):765-74. doi: 10.1093/jaoac/94.3.765. [PMID: 21797004]
  • Ryh-Nan Pan, Cheng-Huei Hsiong, Pei-Wei Huang, Wei-Shiuan Tsai, Wen-Yi Li, Li-Heng Pao. Simultaneous quantification of triazolam and its metabolites in human urine by liquid chromatography-tandem mass spectrometry. Journal of analytical toxicology. 2011 Apr; 35(3):170-5. doi: 10.1093/anatox/35.3.170. [PMID: 21439153]
  • Joseph J Raybon, Devin Pray, Daniel G Morgan, Mary Zoeckler, Ming Zheng, Michael Sinz, Sean Kim. Pharmacokinetic-pharmacodynamic modeling of rifampicin-mediated Cyp3a11 induction in steroid and xenobiotic X receptor humanized mice. The Journal of pharmacology and experimental therapeutics. 2011 Apr; 337(1):75-82. doi: 10.1124/jpet.110.176677. [PMID: 21205914]
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  • Radim Vrzal, Katerina Kubesova, Petr Pavek, Zdenek Dvorak. Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines. Toxicology letters. 2010 Mar; 193(2):183-8. doi: 10.1016/j.toxlet.2010.01.004. [PMID: 20080160]
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