Levocabastine (BioDeep_00000018173)

   

human metabolite blood metabolite Chemicals and Drugs


代谢物信息卡片


(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid

化学式: C26H29FN2O2 (420.22129459999996)
中文名称: 左卡巴司丁, 卡巴斯汀
谱图信息: 最多检出来源 Homo sapiens(blood) 3.06%

分子结构信息

SMILES: CC1CN(C2CCC(C#N)(c3ccc(F)cc3)CC2)CCC1(C(=O)O)c1ccccc1
InChI: InChI=1S/C26H29FN2O2/c1-19-17-29(16-15-26(19,24(30)31)21-5-3-2-4-6-21)23-11-13-25(18-28,14-12-23)20-7-9-22(27)10-8-20/h2-10,19,23H,11-17H2,1H3,(H,30,31)/t19-,23?,25?,26-/m1/s1

描述信息

Levocabastine is only found in individuals that have used or taken this drug. It is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979.Levocabastine is a potent, selective histamine H1-receptor antagonist. It works by competing with histamine for H1-receptor sites on effector cells. It thereby prevents, but does not reverse, responses mediated by histamine alone. Levocabastine does not block histamine release but, rather, prevents histamine binding and activity. Levocabastine also binds neurotensin 2 receptors and serves as a neurotensin agonist. This can induce some degree of analgesia.
R - Respiratory system > R01 - Nasal preparations > R01A - Decongestants and other nasal preparations for topical use > R01AC - Antiallergic agents, excl. corticosteroids
D018377 - Neurotransmitter Agents > D018494 - Histamine Agents > D006633 - Histamine Antagonists
S - Sensory organs > S01 - Ophthalmologicals > S01G - Decongestants and antiallergics
C308 - Immunotherapeutic Agent > C29578 - Histamine-1 Receptor Antagonist

同义名列表

18 个代谢物同义名

(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid; 1-(4-Cyano-4-(4-fluorophenyl)cyclohexyl)-3-methyl-4-phenyl-4-piperidinecarboxylic acid; Ciba vision brand OF levocabastine hydrochloride; Taxandria brand OF levocabastine hydrochloride; Janssen brand OF levocabastine hydrochloride; Chauvin brand OF levocabastine hydrochloride; Esteve brand OF levocabastine hydrochloride; Winzer brand OF levocabastine hydrochloride; Iolab brand OF levocabastine hydrochloride; Levocabastine hydrochloride; Levocabastine; Levocabastin; Cabastine; Livostin; Lévophta; Levophta; Livocab; Bilina



数据库引用编号

12 个数据库交叉引用编号

分类词条

相关代谢途径

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代谢反应

0 个相关的代谢反应过程信息。

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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

  • Fahad M Almutairi, Mohammad Rehan Ajmal, Mohammad Khursheed Siddiqi, Nabeela Majid, Adel Ibrahim Ahmad Al-Alawy, Ali Saber Abdelhameed, Rizwan Hasan Khan. Biophysical insight into the interaction of levocabastine with human serum albumin: spectroscopy and molecular docking approach. Journal of biomolecular structure & dynamics. 2021 Mar; 39(5):1525-1534. doi: 10.1080/07391102.2020.1750486. [PMID: 32308140]
  • Ann Allen, Robert D Murdoch, Philippe Bareille, Olivia Burns, Stephen Hughes, Ashutosh Gupta, Sam R Miller. Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination. Clinical pharmacology in drug development. 2016 May; 5(3):225-31. doi: 10.1002/cpdd.218. [PMID: 27163502]
  • Tadafumi Tamura. Olopatadine ophthalmic solution suppresses substance P release in the conjunctivitis models. Asia Pacific allergy. 2012 Apr; 2(2):115-21. doi: 10.5415/apallergy.2012.2.2.115. [PMID: 22701861]
  • Jacek Piątek, Paweł Maćkowiak, Hanna Krauss, Dorota Nowak, Paweł Bogdański. In vivo investigations of neurotensin receptors in adipocytes, hepatocytes and enterocytes of rat. Annals of agricultural and environmental medicine : AAEM. 2011; 18(2):433-6. doi: ". [PMID: 22216825]
  • Sophie Béraud-Dufour, Amar Abderrahmani, Jacques Noel, Frédéric Brau, Gérard Waeber, Jean Mazella, Thierry Coppola. Neurotensin is a regulator of insulin secretion in pancreatic beta-cells. The international journal of biochemistry & cell biology. 2010 Oct; 42(10):1681-8. doi: 10.1016/j.biocel.2010.06.018. [PMID: 20601081]
  • George B Lenon, Charlie C L Xue, David F Story, Frank C K Thien, Sarah McPhee, Chun G Li. Inhibition of release of inflammatory mediators in primary and cultured cells by a Chinese herbal medicine formula for allergic rhinitis. Chinese medicine. 2007 Feb; 2(?):2. doi: 10.1186/1749-8546-2-2. [PMID: 17302969]
  • Yoshihiro Dake, Tadao Enomoto, Lei Cheng, Keisuke Enomoto, Akira Shibano, Hiroki Ikeda, Shigetoshi Yoda, Shinji Yajin, Takema Sakota, Emi Yamanishi. Effect of antihistamine eye drops on the conjunctival provocation test with Japanese cedar pollen allergen. Allergology international : official journal of the Japanese Society of Allergology. 2006 Dec; 55(4):373-8. doi: 10.2332/allergolint.55.373. [PMID: 17130679]
  • Amélie Perron, Philippe Sarret, Louis Gendron, Thomas Stroh, Alain Beaudet. Identification and functional characterization of a 5-transmembrane domain variant isoform of the NTS2 neurotensin receptor in rat central nervous system. The Journal of biological chemistry. 2005 Mar; 280(11):10219-27. doi: 10.1074/jbc.m410557200. [PMID: 15637074]
  • Rena Yamauchi, Kousaku Ohinata, Masaaki Yoshikawa. Beta-lactotensin and neurotensin rapidly reduce serum cholesterol via NT2 receptor. Peptides. 2003 Dec; 24(12):1955-61. doi: 10.1016/j.peptides.2003.10.003. [PMID: 15127948]
  • C Blondin, B Cholley, N Haeffner-Cavaillon, P Goldschmidt. [In vitro effects of antiallergic eyedrops on complement activation induced by particulate matter]. Journal francais d'ophtalmologie. 2003 Apr; 26(4):328-36. doi: . [PMID: 12843888]
  • Ha Minh Ky Nguyen, Catherine M Cahill, Peter S McPherson, Alain Beaudet. Receptor-mediated internalization of [3H]-neurotensin in synaptosomal preparations from rat neostriatum. Neuropharmacology. 2002 Jun; 42(8):1089-98. doi: 10.1016/s0028-3908(02)00054-0. [PMID: 12128010]
  • Y Sugimoto, Y Iba, K Ishizawa, G Suzuki, C Kamei. Effects of levocabastine on lipid mediator release from guinea pig lung fragments. Acta medica Okayama. 1999 Dec; 53(6):271-4. doi: 10.18926/amo/31623. [PMID: 10631382]
  • M Goulet, M Morissette, R Grondin, P Falardeau, P J Bédard, W Rostène, T Di Paolo. Neurotensin receptors and dopamine transporters: effects of MPTP lesioning and chronic dopaminergic treatments in monkeys. Synapse (New York, N.Y.). 1999 Jun; 32(3):153-64. doi: 10.1002/(sici)1098-2396(19990601)32:3<153::aid-syn2>3.0.co;2-x. [PMID: 10340626]
  • J Corren, G Rachelefsky, S Spector, H Schanker, S Siegel, D Holton, K Karcher, S Travers. Onset and duration of action of levocabastine nasal spray in atopic patients under nasal challenge conditions. The Journal of allergy and clinical immunology. 1999 Apr; 103(4):574-80. doi: 10.1016/s0091-6749(99)70226-5. [PMID: 10200003]
  • L Pesco-Koplowitz, A Hassell, P Lee, H Zhou, N Hall, B Wiesinger, W Mechlinski, M Grover, T Hunt, R Smith, S Travers. Lack of effect of erythromycin and ketoconazole on the pharmacokinetics and pharmacodynamics of steady-state intranasal levocabastine. Journal of clinical pharmacology. 1999 Jan; 39(1):76-85. doi: 10.1177/00912709922007589. [PMID: 9987703]
  • C Svensson, M Andersson, L Greiff, L O Blychert, C G Persson. Effects of topical budesonide and levocabastine on nasal symptoms and plasma exudation responses in seasonal allergic rhinitis. Allergy. 1998 Apr; 53(4):367-74. doi: 10.1111/j.1398-9995.1998.tb03907.x. [PMID: 9574878]
  • D Nouel, M P Faure, J A St Pierre, R Alonso, R Quirion, A Beaudet. Differential binding profile and internalization process of neurotensin via neuronal and glial receptors. The Journal of neuroscience : the official journal of the Society for Neuroscience. 1997 Mar; 17(5):1795-803. doi: 10.1523/jneurosci.17-05-01795.1997. [PMID: 9030638]
  • S Noble, D McTavish. Levocabastine. An update of its pharmacology, clinical efficacy and tolerability in the topical treatment of allergic rhinitis and conjunctivitis. Drugs. 1995 Dec; 50(6):1032-49. doi: 10.2165/00003495-199550060-00009. [PMID: 8612470]
  • J Heykants, A Van Peer, V Van de Velde, E Snoeck, W Meuldermans, R Woestenborghs. The pharmacokinetic properties of topical levocabastine. A review. Clinical pharmacokinetics. 1995 Oct; 29(4):221-30. doi: 10.2165/00003088-199529040-00002. [PMID: 8549024]
  • J Zazgornik, M L Huang, A Van Peer, R Woestenborghs, J Heykants, A Stephen. Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency. Journal of clinical pharmacology. 1993 Dec; 33(12):1214-8. doi: 10.1002/j.1552-4604.1993.tb03922.x. [PMID: 7907347]
  • K Tasaka, C Kamei, M Akagi, M Mio, T Shirasaka, M Chokki. Antiallergic profile of the novel H1-antihistaminic compound levocabastine. Arzneimittel-Forschung. 1993 Dec; 43(12):1331-7. doi: ". [PMID: 7511378]
  • U Pipkorn, M Bende, J Hedner, T Hedner. A double-blind evaluation of topical levocabastine, a new specific H1 antagonist in patients with allergic conjunctivitis. Allergy. 1985 Oct; 40(7):491-6. doi: 10.1111/j.1398-9995.1985.tb00255.x. [PMID: 2866725]