Olopatadine Hydrochloride (BioDeep_00000015235)

   


代谢物信息卡片


Olopatadine Hydrochloride

化学式: C21H24ClNO3 (373.14446240000007)
中文名称: 盐酸奥洛他定
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CN(C)CCC=C1C2=CC=CC=C2COC3=C1C=C(C=C3)CC(=O)O.Cl
InChI: 1H/b18-8-

描述信息

D018377 - Neurotransmitter Agents > D018494 - Histamine Agents > D006633 - Histamine Antagonists
D018373 - Peripheral Nervous System Agents > D018689 - Sensory System Agents
C308 - Immunotherapeutic Agent > C29578 - Histamine-1 Receptor Antagonist
D002491 - Central Nervous System Agents > D000700 - Analgesics
D000893 - Anti-Inflammatory Agents
D018501 - Antirheumatic Agents
D018926 - Anti-Allergic Agents
Olopatadine hydrochloride (ALO4943A) is a histamine blocker used to treat allergic conjunctivitis. Target: Histamine Receptor Olopatadine hydrochloride (ALO4943A) is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine hydrochloride (ALO4943A) significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine hydrochloride (ALO4943A) was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of Olopatadine hydrochloride (ALO4943A) accounted for not less than 58\% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine hydrochloride (ALO4943A) is one of the few renal clearance drugs in antiallergic drugs. Olopatadine hydrochloride (ALO4943A) was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. Olopatadine hydrochloride (ALO4943A) inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by Olopatadine hydrochloride (ALO4943A) applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067\% and 0.0170\%, w/v, respectively) [3].

同义名列表

4 个代谢物同义名

Olopatadine Hydrochloride; ALO4943A; KW4679; Olopatadine (hydrochloride)



数据库引用编号

9 个数据库交叉引用编号

分类词条

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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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  • 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。

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文献列表

  • Büşra Çalışkan, Yeliz Demir, Cüneyt Türkeş. Ophthalmic drugs: in vitro paraoxonase 1 inhibition and molecular docking studies. Biotechnology and applied biochemistry. 2022 Dec; 69(6):2273-2283. doi: 10.1002/bab.2284. [PMID: 34786760]
  • Taisuke Kuroda, Shun-Ichi Nagata, Norihisa Tamura, Hiroshi Mita, Kanichi Kusano, Fumiaki Mizobe, Yoshimasa Takizawa, Kentaro Fukuda, Yoshinori Kasashima. Pharmacokinetics and pharmacodynamics of olopatadine following administration via nasogastric tube to healthy horses. American journal of veterinary research. 2019 Jul; 80(7):689-695. doi: 10.2460/ajvr.80.7.689. [PMID: 31246121]
  • Prasanthi Polamreddy, Vinita Vishwakarma, Puneet Saxena. Identification of potential anti-hepatitis C virus agents targeting non structural protein 5B using computational techniques. Journal of cellular biochemistry. 2018 11; 119(10):8574-8587. doi: 10.1002/jcb.27071. [PMID: 30058078]
  • Piyush Patel, Anne Marie Salapatek, Ravi S Talluri, Sudeesh K Tantry. Pharmacokinetics of intranasal mometasone in the fixed-dose combination GSP301 versus two monotherapy intranasal mometasone formulations. Allergy and asthma proceedings. 2018 May; 39(3):232-239. doi: 10.2500/aap.2018.39.4134. [PMID: 29669668]
  • Piyush Patel, Anne Marie Salapatek, Ravi S Talluri, Sudeesh K Tantry. Pharmacokinetics of intranasal olopatadine in the fixed-dose combination GSP301 versus two monotherapy intranasal olopatadine formulations. Allergy and asthma proceedings. 2018 May; 39(3):224-231. doi: 10.2500/aap.2018.39.4133. [PMID: 29669667]
  • Kayoko Kanamitsu, Yoshitane Nozaki, Yoko Nagaya, Yuichi Sugiyama, Hiroyuki Kusuhara. Quantitative prediction of histamine H1 receptor occupancy by the sedative and non-sedative antagonists in the human central nervous system based on systemic exposure and preclinical data. Drug metabolism and pharmacokinetics. 2017 Apr; 32(2):135-144. doi: 10.1016/j.dmpk.2016.11.007. [PMID: 28190755]
  • Ganesh R Iyer, Marita M Cason, Scott W Womble, Guangming Li, James E Chastain. Ocular pharmacokinetics comparison between 0.2\% olopatadine and 0.77\% olopatadine hydrochloride ophthalmic solutions administered to male New Zealand white rabbits. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics. 2015 May; 31(4):204-10. doi: 10.1089/jop.2014.0140. [PMID: 25775192]
  • Asuka Baba, Masahiro Tachi, Yoshio Maruyama, Itsuro Kazama. Olopatadine inhibits exocytosis in rat peritoneal mast cells by counteracting membrane surface deformation. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2015; 35(1):386-96. doi: 10.1159/000369704. [PMID: 25591779]
  • Ayuko Matsushita, Masahiro Seike, Haruka Okawa, Yayoi Kadawaki, Hiroshi Ohtsu. Advantages of histamine H4 receptor antagonist usage with H1 receptor antagonist for the treatment of murine allergic contact dermatitis. Experimental dermatology. 2012 Sep; 21(9):714-5. doi: 10.1111/j.1600-0625.2012.01559.x. [PMID: 22897580]
  • Ping Zhu, Yu-Guan Wen, Xiao-Ping Fan, Zhi-Ling Zhou, Rui-Xin Fan, Ji-Mei Chen, Ke-Li Huang, Xiao-Lan Zhu, Yan-Fang Chen, Jian Zhuang. A rapid and sensitive liquid chromatography-tandem mass spectrometry method for determination of olopatadine concentration in human plasma. Journal of analytical toxicology. 2011 Mar; 35(2):113-8. doi: 10.1093/anatox/35.2.113. [PMID: 21396231]
  • Hideyuki Yamamoto, Takechiyo Yamada, Seita Kubo, Yoko Osawa, Yuichi Kimura, Myonmi Oh, Dai Susuki, Tetsuji Takabayashi, Masayuki Okamoto, Shigeharu Fujieda. Efficacy of oral olopatadine hydrochloride for the treatment of seasonal allergic rhinitis: A randomized, double-blind, placebo-controlled study. Allergy and asthma proceedings. 2010 Jul; 31(4):296-303. doi: 10.2500/aap.2010.31.3355. [PMID: 20819319]
  • Hiroyuki Murota, Mostafa Abd El-latif, Tadafumi Tamura, Toru Amano, Ichiro Katayama. Olopatadine hydrochloride improves dermatitis score and inhibits scratch behavior in NC/Nga mice. International archives of allergy and immunology. 2010; 153(2):121-32. doi: 10.1159/000312629. [PMID: 20407268]
  • Chisato Hosokawa, Satoshi Takeuchi, Masutaka Furue. Severity scores, itch scores and plasma substance P levels in atopic dermatitis treated with standard topical therapy with oral olopatadine hydrochloride. The Journal of dermatology. 2009 Apr; 36(4):185-90. doi: 10.1111/j.1346-8138.2009.00621.x. [PMID: 19348655]
  • Junko Yamaguchi, Michiko Aihara, Yusuke Kobayashi, Takeshi Kambara, Zenro Ikezawa. Quantitative analysis of nerve growth factor (NGF) in the atopic dermatitis and psoriasis horny layer and effect of treatment on NGF in atopic dermatitis. Journal of dermatological science. 2009 Jan; 53(1):48-54. doi: 10.1016/j.jdermsci.2008.08.011. [PMID: 18922683]
  • Nan-Nan Chu, Wei-Li Chen, Hong-Rong Xu, Xue-Ning Li. Pharmacokinetics of orally administered single- and multiple-dose olopatadine in healthy Chinese subjects: an open-label study. Clinical drug investigation. 2009; 29(7):451-457. doi: 10.2165/00044011-200929070-00003. [PMID: 19499962]
  • Motoo Kikuchi, Toshiaki Inagaki, Hidekazu Hanaki, Shinsuke Harada, Ryuzo Ueda. Effects of olopatadine in limited scleroderma with peripheral eosinophils. Geriatrics & gerontology international. 2008 Sep; 8(3):204-8. doi: 10.1111/j.1447-0594.2008.00471.x. [PMID: 18822005]
  • Nobuhito Mimura, Yoshinori Nagata, Takashi Kuwabara, Nobuo Kubo, Eiichi Fuse. P-glycoprotein limits the brain penetration of olopatadine hydrochloride, H1-receptor antagonist. Drug metabolism and pharmacokinetics. 2008; 23(2):106-14. doi: 10.2133/dmpk.23.106. [PMID: 18445990]
  • Manabu Tashiro, Hideki Mochizuki, Yumiko Sakurada, Kenji Ishii, Keiichi Oda, Yuichi Kimura, Toru Sasaki, Kiichi Ishiwata, Kazuhiko Yanai. Brain histamine H receptor occupancy of orally administered antihistamines measured by positron emission tomography with (11)C-doxepin in a placebo-controlled crossover study design in healthy subjects: a comparison of olopatadine and ketotifen. British journal of clinical pharmacology. 2006 Jan; 61(1):16-26. doi: 10.1111/j.1365-2125.2005.02514.x. [PMID: 16390347]
  • Kunio Izu, Yoshiki Tokura. The various effects of four H1-antagonists on serum substance P levels in patients with atopic dermatitis. The Journal of dermatology. 2005 Oct; 32(10):776-81. doi: 10.1111/j.1346-8138.2005.tb00844.x. [PMID: 16361727]
  • Hirotoshi Furukawa, Masanobu Takahashi, Koichiro Nakamura, Fumio Kaneko. Effect of an antiallergic drug (Olopatadine hydrochloride) on TARC/CCL17 and MDC/CCL22 production by PBMCs from patients with atopic dermatitis. Journal of dermatological science. 2004 Dec; 36(3):165-72. doi: 10.1016/j.jdermsci.2004.09.001. [PMID: 15541638]
  • Masahiro Matsubara, Shigehiro Masaki, Kenji Ohmori, Akira Karasawa, Kazuhide Hasegawa. Differential regulation of IL-4 expression and degranulation by anti-allergic olopatadine in rat basophilic leukemia (RBL-2H3) cells. Biochemical pharmacology. 2004 Apr; 67(7):1315-26. doi: 10.1016/j.bcp.2003.12.008. [PMID: 15013847]
  • Kenji Ohmori, Kazuhide Hasegawa, Tadafumi Tamura, Kiyomi Miyake, Masahiro Matsubara, Shigehiro Masaki, Akira Karasawa, Naoko Urayama, Kaori Horikoshi, Jiro Kajita, Masanori Hasegawa, Koji Taniguchi, Toshio Komada, Yuji Kawamoto. Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. Arzneimittel-Forschung. 2004; 54(12):809-29. doi: 10.1055/s-0031-1297036. [PMID: 15646365]
  • 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]
  • Kenji Ohmori, Ken-ichi Hayashi, Toshihiko Kaise, Etsuo Ohshima, Satoshi Kobayashi, Takashi Yamazaki, Akimichi Mukouyama. Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Japanese journal of pharmacology. 2002 Apr; 88(4):379-97. doi: 10.1254/jjp.88.379. [PMID: 12046981]
  • K Hayashi, T Kaise, K Ohmori, A Ishii, A Karasawa. Effects of olopatadine hydrochloride on the cutaneous vascular hyperpermeability and the scratching behavior induced by poly-L-arginine in rats. Japanese journal of pharmacology. 2001 Oct; 87(2):167-70. doi: 10.1254/jjp.87.167. [PMID: 11700017]
  • K Ohmori, T Ikemura, H Kobayashi, A Mukouyama. [Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug]. Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 2001 Jul; 118(1):51-8. doi: 10.1254/fpj.118.51. [PMID: 11496828]
  • H Brockman, G Graff, J Spellman, J Yanni. A comparison of the effects of olopatadine and ketotifen on model membranes. Acta ophthalmologica Scandinavica. Supplement. 2000; ?(230):10-5. doi: 10.1034/j.1600-0420.2000.078s230010.x. [PMID: 11057342]
  • K Fujita, H Magara, H Kobayashi. Determination of olopatadine, a new antiallergic agent, and its metabolites in human plasma by high-performance liquid chromatography with electrospray ionization tandem mass spectrometry. Journal of chromatography. B, Biomedical sciences and applications. 1999 Aug; 731(2):345-52. doi: 10.1016/s0378-4347(99)00236-4. [PMID: 10510789]
  • T Tateishi, S Kobayashi, C Shigeyama, T Nakamura, H Kobayashi. Pharmacokinetics of KW-4679 in the elderly: single-dose and multiple-dose trials. Drugs under experimental and clinical research. 1998; 24(1):1-7. doi: NULL. [PMID: 9604143]
  • T Ikemura, H Manabe, Y Sasaki, H Ishii, K Onuma, I Miki, H Kase, S Sato, S Kitamura, K Ohmori. KW-4679, an antiallergic drug, inhibits the production of inflammatory lipids in human polymorphonuclear leukocytes and guinea pig eosinophils. International archives of allergy and immunology. 1996 May; 110(1):57-63. doi: 10.1159/000237311. [PMID: 8645979]
  • E Ohshima, H Sato, H Obase, T Uchimura, T Kuwabara, S Kobayashi. Synthesis of a dibenz[b,e]oxepin-bovine serum albumin conjugate for radioimmunoassay of KW-4679 ((Z)-11-[3-(dimethylamino)propylidene]-6,11- dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride). Chemical & pharmaceutical bulletin. 1992 Sep; 40(9):2552-4. doi: 10.1248/cpb.40.2552. [PMID: 1446376]