Afoxolaner (BioDeep_00000175774)

   

human metabolite blood metabolite


代谢物信息卡片


2-[(4-{5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl}naphthalen-1-yl)formamido]-N-(2,2,2-trifluoroethyl)ethanimidic acid

化学式: C26H17ClF9N3O3 (625.081467)
中文名称: 阿福拉纳
谱图信息: 最多检出来源 Homo sapiens(blood) 75%

分子结构信息

SMILES: C1C(=NOC1(C2=CC(=CC(=C2)Cl)C(F)(F)F)C(F)(F)F)C3=CC=C(C4=CC=CC=C43)C(=O)NCC(=O)NCC(F)(F)F
InChI: InChI=1S/C26H17ClF9N3O3/c27-15-8-13(7-14(9-15)25(31,32)33)23(26(34,35)36)10-20(39-42-23)18-5-6-19(17-4-2-1-3-16(17)18)22(41)37-11-21(40)38-12-24(28,29)30/h1-9H,10-12H2,(H,37,41)(H,38,40)

描述信息

C254 - Anti-Infective Agent > C276 - Antiparasitic Agent
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod[1][2].

同义名列表

7 个代谢物同义名

2-[(4-{5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl}naphthalen-1-yl)formamido]-N-(2,2,2-trifluoroethyl)ethanimidic acid; 4-(5-(3-Chloro-5-(trifluoromethyl)-phenyl)-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl)-N-(2- oxo-2-((2,2,2-trifluoroethyl)amino)ethyl-1-naphthalenecarboxamide; 2-[(4-{5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl}naphthalen-1-yl)formamido]-N-(2,2,2-trifluoroethyl)ethanimidate; 2-[(4-{5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl}naphthalen-1-yl)formamido]-N-(2,2,2-trifluoroethyl)ethanimidic acid; Afoxolaner; AH252723; a1443



数据库引用编号

8 个数据库交叉引用编号

分类词条

相关代谢途径

Reactome(0)

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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

  • Kristina Kryda, Sean P Mahabir, Tammy Inskeep, Jady Rugg. Safety and efficacy of a novel oral chewable combination tablet containing sarolaner, moxidectin and pyrantel (Simparica Trio™) against natural flea infestations in client-owned dogs in the USA. Parasites & vectors. 2020 Mar; 13(1):98. doi: 10.1186/s13071-020-3952-3. [PMID: 32113472]
  • Charlotte Bernigaud, Fang Fang, Katja Fischer, Anne Lespine, Ludwig S Aho, Amanda J Mullins, Berhane Tecle, Andrew Kelly, Jean-François Sutra, Francis Moreau, Thomas Lilin, Frédéric Beugnet, Françoise Botterel, Olivier Chosidow, Jacques Guillot. Efficacy and Pharmacokinetics Evaluation of a Single Oral Dose of Afoxolaner against Sarcoptes scabiei in the Porcine Scabies Model for Human Infestation. Antimicrobial agents and chemotherapy. 2018 09; 62(9):. doi: 10.1128/aac.02334-17. [PMID: 29914951]
  • Jessica M Abbate, Ettore Napoli, Francesca Arfuso, Gabriella Gaglio, Salvatore Giannetto, Lenaig Halos, Frederic Beugnet, Emanuele Brianti. Six-month field efficacy and safety of the combined treatment of dogs with Frontline Tri-Act® and NexGard Spectra®. Parasites & vectors. 2018 Jul; 11(1):425. doi: 10.1186/s13071-018-2957-7. [PMID: 30012179]
  • M Drag, J Saik, J Harriman, L Letendre, S Yoon, D Larsen. Safety evaluation of orally administered afoxolaner and milbemycin oxime in eight-week-old dogs. Journal of veterinary pharmacology and therapeutics. 2017 Oct; 40(5):447-453. doi: 10.1111/jvp.12375. [PMID: 27891622]
  • L Letendre, J Harriman, M Drag, A Mullins, T Malinski, S Rehbein. The intravenous and oral pharmacokinetics of afoxolaner and milbemycin oxime when used as a combination chewable parasiticide for dogs. Journal of veterinary pharmacology and therapeutics. 2017 Jan; 40(1):35-43. doi: 10.1111/jvp.12332. [PMID: 27604405]
  • Steffen Rehbein, Martin Knaus, Yasmina Mallouk, Tatjana Breiltgens, Emanuele Brianti, Balázs Capári, Filipe Dantas-Torres, Michel Gau, Anja Joachim, Karl-Heinz Kaulfuß, Zvezdelina Kirkova, Joerg Lechner, Andrei D Mihalca, Rosamaria Mirabito, Saulius Petkevičius, Dhimitër Rapti, Enstela Shukullari, Michel Sedeilhan, Doris Dollhofer, Katrin Kley, Wilfried Lebon, Martin Visser, Philippe Jeannin. Efficacy against nematode infections and safety of afoxolaner plus milbemycin oxime chewable tablets in domestic dogs under field conditions in Europe. Parasitology research. 2017 Jan; 116(1):259-269. doi: 10.1007/s00436-016-5287-8. [PMID: 27771803]
  • Frederic Beugnet, Dionne Crafford, Christa de Vos, Dawid Kok, Diane Larsen, Josephus Fourie. Evaluation of the efficacy of monthly oral administration of afoxolaner plus milbemycin oxime (NexGard Spectra(®), Merial) in the prevention of adult Spirocerca lupi establishment in experimentally infected dogs. Veterinary parasitology. 2016 Aug; 226(?):150-61. doi: 10.1016/j.vetpar.2016.07.002. [PMID: 27514901]
  • Wesley L Shoop, Eric J Hartline, Brandon R Gould, Molly E Waddell, Richard G McDowell, John B Kinney, George P Lahm, Jeffrey K Long, Ming Xu, Ty Wagerle, Gail S Jones, Robert F Dietrich, Daniel Cordova, Mark E Schroeder, Daniel F Rhoades, Eric A Benner, Pat N Confalone. Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs. Veterinary parasitology. 2014 Apr; 201(3-4):179-89. doi: 10.1016/j.vetpar.2014.02.020. [PMID: 24631502]
  • Laura Letendre, Rose Huang, Valerie Kvaternick, Jay Harriman, Marlene Drag, Mark Soll. The intravenous and oral pharmacokinetics of afoxolaner used as a monthly chewable antiparasitic for dogs. Veterinary parasitology. 2014 Apr; 201(3-4):190-7. doi: 10.1016/j.vetpar.2014.02.021. [PMID: 24685320]
  • Marlene Drag, Judith Saik, Jay Harriman, Diane Larsen. Safety evaluation of orally administered afoxolaner in 8-week-old dogs. Veterinary parasitology. 2014 Apr; 201(3-4):198-203. doi: 10.1016/j.vetpar.2014.02.022. [PMID: 24629431]