Lofexidine (BioDeep_00000018469)

   

human metabolite blood metabolite


代谢物信息卡片


2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole

化学式: C11H12Cl2N2O (258.0326642)
中文名称: 洛非西定
谱图信息: 最多检出来源 Homo sapiens(blood) 1.64%

分子结构信息

SMILES: CC(C1=NCCN1)OC2=C(C=CC=C2Cl)Cl
InChI: InChI=1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)

描述信息

Lofexidine is an alpha2-adrenergic receptor agonist. It can be used as a short acting anti-hypertensive, but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. It is approved in the United Kingdom, but is still undergoing clinical trials in the United States.
N - Nervous system > N07 - Other nervous system drugs > N07B - Drugs used in addictive disorders > N07BC - Drugs used in opioid dependence
C78272 - Agent Affecting Nervous System > C29747 - Adrenergic Agent > C87053 - Adrenergic Agonist
D018377 - Neurotransmitter Agents > D018663 - Adrenergic Agents > D000322 - Adrenergic Agonists
D018373 - Peripheral Nervous System Agents > D018689 - Sensory System Agents
D002491 - Central Nervous System Agents > D009292 - Narcotic Antagonists
D002317 - Cardiovascular Agents > D000959 - Antihypertensive Agents
Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].

同义名列表

14 个代谢物同义名

2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole; 2-(1-(2,6-Dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole; 2-(alpha-(2,6-Dichlorophenoxy)ethyl) delta-2-imidazoline; 2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline; 2-(Α-(2,6-dichlorophenoxy)ethyl)2-imidazoline; 2-(a-(2,6-Dichlorophenoxy)ethyl)2-imidazoline; Lofexidine mono-hydrochloride; Lofexidine monohydrochloride; Lofexidine hydrochloride; Lofexidine, (+-)-isomer; Lofexidinum; Lofexidina; Lofexidine; BritLofex



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

  • Constance Guille, Courtney King, Viswanathan Ramakrishnan, Nathaniel Baker, Bernadette Cortese, Lisa Nunn, Taylor Rogers, Aimee McRae-Clark, Kathleen Brady. The impact of lofexidine on stress-related opioid craving and relapse: Design and methodology of a randomized clinical trial. Contemporary clinical trials. 2021 12; 111(?):106616. doi: 10.1016/j.cct.2021.106616. [PMID: 34737091]
  • 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]
  • Gretchen Hermes, Scott M Hyman, Nia Fogelman, Thomas R Kosten, Rajita Sinha. Lofexidine in Combination With Oral Naltrexone for Opioid Use Disorder Relapse Prevention: A Pilot Randomized, Double-Blind, Placebo-Controlled Study. The American journal on addictions. 2019 11; 28(6):480-488. doi: 10.1111/ajad.12942. [PMID: 31448846]
  • Fergus D Law, Alison M Diaper, Jan K Melichar, Simon Coulton, David J Nutt, Judy S Myles. Buprenorphine/naloxone versus methadone and lofexidine in community stabilisation and detoxification: A randomised controlled trial of low dose short-term opiate-dependent individuals. Journal of psychopharmacology (Oxford, England). 2017 08; 31(8):1046-1055. doi: 10.1177/0269881117711710. [PMID: 28631527]
  • Laura Sheard, Nat M J Wright, Clive E Adams, Nicole Bound, Bruno Rushforth, Roger Hart, Charlotte N E Tompkins. The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) Prisons Project Study: protocol for a randomised controlled trial comparing methadone and buprenorphine for opiate detoxification. Trials. 2009 Jul; 10(?):53. doi: 10.1186/1745-6215-10-53. [PMID: 19602218]
  • John Schmittner, Jennifer R Schroeder, David H Epstein, Mori J Krantz, Nicole C Eid, Kenzie L Preston. Electrocardiographic effects of lofexidine and methadone coadministration: secondary findings from a safety study. Pharmacotherapy. 2009 May; 29(5):495-502. doi: 10.1592/phco.29.5.495. [PMID: 19397459]
  • Laura Sheard, Nat M J Wright, Hany G El-Sayeh, Clive E Adams, Ryan Li, Charlotte N E Tompkins. The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) prisons project: a randomised controlled trial comparing dihydrocodeine and buprenorphine for opiate detoxification. Substance abuse treatment, prevention, and policy. 2009 Feb; 4(?):1. doi: 10.1186/1747-597x-4-1. [PMID: 19196468]
  • Abeer M Al Ghananeem, Barbara H Herman, Maggie Abbassi, Elmer Yu, Karen Miotto, Charles P O'Brien, Walter Ling, Ann Montgomery, Robert Walsh. Urine and plasma pharmacokinetics of lofexidine after oral delivery in opiate-dependent patients. The American journal of drug and alcohol abuse. 2009; 35(5):311-5. doi: 10.1080/00952990903060135. [PMID: 19637105]
  • Xue Wang, Jing Li, Mingsheng Huang, Lin Kang, Min Hu. A study on Fu-Yuan Pellet, a traditional chinese medicine formula for detoxification of heroin addictions. The American journal of drug and alcohol abuse. 2009; 35(6):408-11. doi: 10.3109/00952990903377146. [PMID: 20014908]
  • Elmer Yu, Karen Miotto, Evaristo Akerele, Charles P O'Brien, Walter Ling, Herbert Kleber, Marian W Fischman, Ahmed Elkashef, Barbara H Herman, Abeer M Al-Ghananeem. Clinical pharmacokinetics of lofexidine, the alpha 2-adrenergic receptor agonist, in opiate addicts plasma using a highly sensitive liquid chromatography tandem mass spectrometric analysis. The American journal of drug and alcohol abuse. 2008; 34(5):611-6. doi: 10.1080/00952990802308122. [PMID: 18821454]
  • Jie Shi, Guo-Zhu Xu, Ting-Ting Liu, Xi Wang, Li-Yang Shen, Jing Li, Wei Hao, Hong-Xian Chen, Su-Xia Li, Lin Lu. A comparative clinical study of the effects of the traditional Chinese medicine Jinniu capsules and lofexidine on acute heroin withdrawal symptoms. The American journal of drug and alcohol abuse. 2008; 34(6):792-800. doi: 10.1080/00952990802491563. [PMID: 19016185]
  • Lin Kang, Bing Li, Lei Gao, Suxia Li, Dan Wang, Min Hu, Jing Li. Tai-Kang-Ning, a Chinese herbal medicine formula, alleviates acute heroin withdrawal. The American journal of drug and alcohol abuse. 2008; 34(3):269-76. doi: 10.1080/00952990802013409. [PMID: 18428069]
  • Nat M J Wright, Laura Sheard, Charlotte N E Tompkins, Clive E Adams, Victoria L Allgar, Nicola S Oldham. Buprenorphine versus dihydrocodeine for opiate detoxification in primary care: a randomised controlled trial. BMC family practice. 2007 Jan; 8(?):3. doi: 10.1186/1471-2296-8-3. [PMID: 17210079]
  • Laura Sheard, Clive E Adams, Nat M J Wright, Hany El-Sayeh, Richard Dalton, Charlotte N E Tompkins. The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) prisons project pilot study: protocol for a randomised controlled trial comparing dihydrocodeine and buprenorphine for opiate detoxification. Trials. 2007 Jan; 8(?):1. doi: 10.1186/1745-6215-8-1. [PMID: 17210080]
  • Yi-Lang Tang, Dong Zhao, Chengzheng Zhao, Joseph F Cubells. Opiate addiction in China: current situation and treatments. Addiction (Abingdon, England). 2006 May; 101(5):657-65. doi: 10.1111/j.1360-0443.2006.01367.x. [PMID: 16669899]
  • Ihsan Ergün, M Cenk Akbostanci, Başol Canbakan, Bilge Koçer, Arzu Ensari, Gökhan Nergizoglu, Kenan Keven. Minimal change nephrotic syndrome with stiff-person syndrome: is there a link?. American journal of kidney diseases : the official journal of the National Kidney Foundation. 2005 Jul; 46(1):e11-4. doi: 10.1053/j.ajkd.2005.03.009. [PMID: 15983949]
  • Nicola S Oldham, Nat M J Wright, Clive E Adams, Laura Sheard, Charlotte N E Tompkins. The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) project: an open-label pragmatic randomised control trial comparing the efficacy of differing therapeutic agents for primary care detoxification from either street heroin or methadone [ISRCTN07752728]. BMC family practice. 2004 Apr; 5(?):9. doi: 10.1186/1471-2296-5-9. [PMID: 15117415]
  • De-bin Huang, Zhao-fen Yu, Lin Fu. [Clinical observation on effect of modified banxia houpu decoction in treating patients with protracted heroin abstinence syndrome]. Zhongguo Zhong xi yi jie he za zhi Zhongguo Zhongxiyi jiehe zazhi = Chinese journal of integrated traditional and Western medicine. 2004 Mar; 24(3):216-9. doi: ". [PMID: 15074088]
  • Hugues Greney, Dragan Urosevic, Stephan Schann, Laurence Dupuy, Véronique Bruban, Jean-Daniel Ehrhardt, Pascal Bousquet, Monique Dontenwill. [125I]2-(2-chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a high-affinity radioligand selective for I1 imidazoline receptors. Molecular pharmacology. 2002 Jul; 62(1):181-91. doi: 10.1124/mol.62.1.181. [PMID: 12065769]
  • Ming Li, Kevin Chen, Zhixian Mo. Use of qigong therapy in the detoxification of heroin addicts. Alternative therapies in health and medicine. 2002 Jan; 8(1):50-4, 56. doi: ". [PMID: 11795622]
  • G Gerra, A Zaimovic, F Giusti, C Di Gennaro, U Zambelli, S Gardini, R Delsignore. Lofexidine versus clonidine in rapid opiate detoxification. Journal of substance abuse treatment. 2001 Jul; 21(1):11-7. doi: 10.1016/s0740-5472(01)00178-7. [PMID: 11516922]
  • P Cushman, J R Sowers. Alcohol withdrawal syndrome: clinical and hormonal responses to alpha 2-adrenergic agonist treatment. Alcoholism, clinical and experimental research. 1989 Jun; 13(3):361-4. doi: 10.1111/j.1530-0277.1989.tb00336.x. [PMID: 2568765]
  • N D Vlachakis, M Velasquez, N Alexander, R F Maronde. Hemodynamic effect of lofexidine with a diuretic in hypertension. Clinical pharmacology and therapeutics. 1983 Dec; 34(6):764-9. doi: 10.1038/clpt.1983.247. [PMID: 6357591]
  • I Midgley, A G Fowkes, L F Chasseaud, D R Hawkins, R Girkin, K Kesselring. Biotransformation of lofexidine in humans. Xenobiotica; the fate of foreign compounds in biological systems. 1983 Feb; 13(2):87-95. doi: 10.3109/00498258309052241. [PMID: 6880242]
  • T C Fagan, S S Bloomfield, T D Cowart, R H Corns-Hurwitz, R J Lipicky, E C Conradi, C Y Hsu, W J Grossman, G E Harmon, W J Degenhart, A W Sinkfield, T E Gaffney. Antihypertensive effects of lofexidine in patients with essential hypertension. British journal of clinical pharmacology. 1982 Mar; 13(3):405-10. doi: 10.1111/j.1365-2125.1982.tb01393.x. [PMID: 7059442]
  • H Friehe, R Fontaine, J P Gibson, E J Larson, D M Sells. Toxicology of the combination lofexidine/hydrochlorothiazide. Arzneimittel-Forschung. 1982; 32(8a):966-71. doi: NULL. [PMID: 6890371]
  • B N Garrett, N M Kaplan. Lofexidine in the treatment of hypertension: a twice-daily versus one-daily dose comparison with 24-hour blood pressure monitoring. Journal of clinical pharmacology. 1981 Apr; 21(4):173-80. doi: 10.1002/j.1552-4604.1981.tb05697.x. [PMID: 7016930]
  • F M Fouad, D G Vidt, H Williams, R C Tarazi, E L Bravo. Early hemodynamic and humoral effects of lofexidine. Clinical pharmacology and therapeutics. 1981 Apr; 29(4):498-504. doi: 10.1038/clpt.1981.69. [PMID: 7471616]
  • J Mehta, P Mehta. Platelet function in hypertension and effect of therapy. The American journal of cardiology. 1981 Feb; 47(2):331-4. doi: 10.1016/0002-9149(81)90405-7. [PMID: 6451166]
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