Loxapine (BioDeep_00000002019)

 

Secondary id: BioDeep_00000405887

human metabolite blood metabolite Chemicals and Drugs


代谢物信息卡片


13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0³,⁸]pentadeca-1(11),3,5,7,9,12,14-heptaene

化学式: C18H18ClN3O (327.1138328)
中文名称: 洛沙平
谱图信息: 最多检出来源 Homo sapiens(blood) 95.83%

分子结构信息

SMILES: CN1CCN(C2=NC3=CC=CC=C3OC4=CC=C(Cl)C=C24)CC1
InChI: InChI=1S/C18H18ClN3O/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3

描述信息

Loxapine is only found in individuals that have used or taken this drug. It is an antipsychotic agent used in schizophrenia. [PubChem]Loxapine is a dopamine antagonist, and also a serotonin 5-HT2 blocker. The exact mode of action of Loxapine has not been established, however changes in the level of excitability of subcortical inhibitory areas have been observed in several animal species in association with such manifestations of tranquilization as calming effects and suppression of aggressive behavior.
N - Nervous system > N05 - Psycholeptics > N05A - Antipsychotics > N05AH - Diazepines, oxazepines, thiazepines and oxepines
D002492 - Central Nervous System Depressants > D014149 - Tranquilizing Agents > D014150 - Antipsychotic Agents
D002491 - Central Nervous System Agents > D011619 - Psychotropic Drugs > D014149 - Tranquilizing Agents
D018377 - Neurotransmitter Agents > D015259 - Dopamine Agents > D018492 - Dopamine Antagonists
D002491 - Central Nervous System Agents > D002492 - Central Nervous System Depressants
C78272 - Agent Affecting Nervous System > C29710 - Antipsychotic Agent
Loxapine is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][4].

同义名列表

19 个代谢物同义名

13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0³,⁸]pentadeca-1(11),3,5,7,9,12,14-heptaene; 2-Chloro-11-(4-methyl-1-piperazinyl)-dibenz(b,F)(1,4)oxazepine; 2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,F][1,4]oxazepine; Loxapine monohydrochloride; Hydrochloride, loxapine; Loxapine hydrochloride; Succinate, loxapine; Loxipine succinate; Loxapine succinate; Maleate, loxipine; Loxipine maleate; Loxapinsuccinate; Cloxazepine; Loxapinum; Oxilapine; Loxitane; loxapine; Loxapina; Adasuve



数据库引用编号

17 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

  • Tyler Ruch, Sharon Nuss, Rajashekar Reddy Yeruva, Yonglin Gao, Gulay Tegin, Christina Terrell, Rif S El-Mallakh. Inhaled loxapine for acute agitation in a psychiatric emergency service. Annals of clinical psychiatry : official journal of the American Academy of Clinical Psychiatrists. 2021 08; 33(3):162-167. doi: 10.12788/acp.0032. [PMID: 34398731]
  • 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]
  • Sally Selim, Robert Riesenberg, James Cassella, Jeevan Kunta, Edward Hellriegel, Mark A Smith, Alexander A Vinks, Laura Rabinovich-Guilatt. Pharmacokinetics and Safety of Single-Dose Inhaled Loxapine in Children and Adolescents. Journal of clinical pharmacology. 2017 10; 57(10):1244-1257. doi: 10.1002/jcph.932. [PMID: 28510296]
  • Min Meng, Nan Zhao, Carrie C Pederson, Edward Harrison, Charisse Green, Steven H Gorman, Scott Reuschel. Simultaneous quantification of loxapine, loxapine N-oxide, amoxapine, 8-hydroxyloxapine and 7-hydroxyloxapine in human plasma using LC-MS/MS. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2017 Mar; 1046(?):87-97. doi: 10.1016/j.jchromb.2017.01.007. [PMID: 28152454]
  • Charles V Pollack. Inhaled loxapine for the urgent treatment of acute agitation associated with schizophrenia or bipolar disorder. Current medical research and opinion. 2016 07; 32(7):1253-60. doi: 10.1185/03007995.2016.1170004. [PMID: 27121764]
  • I Jullian-Desayes, A Roselli, C Lamy, M C Alberto-Gondouin, N Janvier, G Venturi-Maestri. Rhabdomyolysis with Acute Renal Failure and Deep Vein Thrombosis Induced by Antipsychotic Drugs: A Case Report. Pharmacopsychiatry. 2015 Nov; 48(7):265-7. doi: 10.1055/s-0035-1564088. [PMID: 26398280]
  • James V Cassella, Daniel A Spyker, Paul P Yeung. A randomized, placebo-controlled repeat-dose thorough QT study of inhaled loxapine in healthy volunteers. International journal of clinical pharmacology and therapeutics. 2015 Nov; 53(11):963-71. doi: NULL. [PMID: 26501204]
  • Daniel A Spyker, Robert A Riesenberg, James V Cassella. Multiple dose pharmacokinetics of inhaled loxapine in subjects on chronic, stable antipsychotic regimens. Journal of clinical pharmacology. 2015 Sep; 55(9):985-94. doi: 10.1002/jcph.502. [PMID: 25808074]
  • A Fernandez, E Dor, M-L Menard, F Askenazy, S Thümmler. [Carbamazepine and psychotropic treatment interaction: Two case studies of carbamazepine overdosage]. Archives de pediatrie : organe officiel de la Societe francaise de pediatrie. 2015 May; 22(5):536-9. doi: 10.1016/j.arcped.2015.02.010. [PMID: 25819631]
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  • Daniel A Spyker, Polina Voloshko, Eugene R Heyman, James V Cassella. Loxapine delivered as a thermally generated aerosol does not prolong QTc in a thorough QT/QTc study in healthy subjects. Journal of clinical pharmacology. 2014 Jun; 54(6):665-74. doi: 10.1002/jcph.257. [PMID: 24375070]
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  • Cho-Ming Loi, Dennis A Smith, Deepak Dalvie. Which metabolites circulate?. Drug metabolism and disposition: the biological fate of chemicals. 2013 May; 41(5):933-51. doi: 10.1124/dmd.112.050278. [PMID: 23454828]
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  • Jennifer S D Zimmer, Shane R Needham, Chad D Christianson, Crystal M Piekarski, Chrystal N Sheaff, Keith Huie, Andrea R Reed, Lori Takahashi. Validation of HPLC-MS/MS methods for analysis of loxapine, amoxapine, 7-OH-loxapine, 8-OH-loxapine and loxapine N-oxide in human plasma. Bioanalysis. 2010 Dec; 2(12):1989-2000. doi: 10.4155/bio.10.156. [PMID: 21110742]
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  • Ming-Hong Hsieh, Wei-Wen Lin, Shao-Tsu Chen, Kao-Ching Chen, Kuang-Peng Chen, Nan-Ying Chiu, Chao Huang, Ching-Jui Chang, Cheng-Hsiu Lin, Te-Jen Lai. A 64-week, multicenter, open-label study of aripiprazole effectiveness in the management of patients with schizophrenia or schizoaffective disorder in a general psychiatric outpatient setting. Annals of general psychiatry. 2010 Sep; 9(?):35. doi: 10.1186/1744-859x-9-35. [PMID: 20849577]
  • Daniel A Spyker, Patrik Munzar, James V Cassella. Pharmacokinetics of loxapine following inhalation of a thermally generated aerosol in healthy volunteers. Journal of clinical pharmacology. 2010 Feb; 50(2):169-79. doi: 10.1177/0091270009347866. [PMID: 19915181]
  • Laura Mercolini, Roberto Mandrioli, Giulia Finizio, Giancarlo Boncompagni, Maria Augusta Raggi. Simultaneous HPLC determination of 14 tricyclic antidepressants and metabolites in human plasma. Journal of separation science. 2010 Jan; 33(1):23-30. doi: 10.1002/jssc.200900493. [PMID: 20091716]
  • Hong Wan, Madeleine Ahman, Anders G Holmén. Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. Journal of medicinal chemistry. 2009 Mar; 52(6):1693-700. doi: 10.1021/jm801441s. [PMID: 19256501]
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  • Linda Hanssens, Gilbert L'Italien, Jean-Yves Loze, Ronald N Marcus, Miranda Pans, Wendy Kerselaers. The effect of antipsychotic medication on sexual function and serum prolactin levels in community-treated schizophrenic patients: results from the Schizophrenia Trial of Aripiprazole (STAR) study (NCT00237913). BMC psychiatry. 2008 Dec; 8(?):95. doi: 10.1186/1471-244x-8-95. [PMID: 19102734]
  • Laura Mercolini, Carolina Colliva, Mario Amore, Salvatore Fanali, Maria Augusta Raggi. HPLC analysis of the antidepressant trazodone and its main metabolite m-CPP in human plasma. Journal of pharmaceutical and biomedical analysis. 2008 Aug; 47(4-5):882-7. doi: 10.1016/j.jpba.2008.02.028. [PMID: 18400445]
  • Alessandro Musenga, Maria Addolorata Saracino, Domenico Spinelli, Egon Rizzato, Giancarlo Boncompagni, Ernst Kenndler, Maria Augusta Raggi. Analysis of the recent antipsychotic aripiprazole in human plasma by capillary electrophoresis and high-performance liquid chromatography with diode array detection. Analytica chimica acta. 2008 Apr; 612(2):204-11. doi: 10.1016/j.aca.2008.02.046. [PMID: 18358867]
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  • Laura Mercolini, Francesca Bugamelli, Ernst Kenndler, Giancarlo Boncompagni, Livia Franchini, Maria Augusta Raggi. Simultaneous determination of the antipsychotic drugs levomepromazine and clozapine and their main metabolites in human plasma by a HPLC-UV method with solid-phase extraction. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2007 Feb; 846(1-2):273-80. doi: 10.1016/j.jchromb.2006.09.019. [PMID: 17045854]
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