1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (BioDeep_00000180228)

   

human metabolite blood metabolite


代谢物信息卡片


1-((5-Chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine

化学式: C14H16ClN3O (277.09818359999997)
中文名称: JNJ-7777120
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CN1CCN(CC1)C(=O)C1=CC2=C(N1)C=CC(Cl)=C2
InChI: InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3

描述信息

JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory[1][2].

同义名列表

4 个代谢物同义名

1-((5-Chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine; 1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine; 5-chloro-2-(4-methylpiperazine-1-carbonyl)-1H-indole; JNJ-7777120



数据库引用编号

8 个数据库交叉引用编号

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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

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文献列表

  • Ahmed F Mohamed, Mohammed F El-Yamany, Fatma A El-Batrawy, Mohamed T Abdel-Aziz. JNJ7777120 Ameliorates Inflammatory and Oxidative Manifestations in a Murine Model of Contact Hypersensitivity via Modulation of TLR and Nrf2 Signaling. Inflammation. 2018 Mar; 41(2):378-389. doi: 10.1007/s10753-017-0693-3. [PMID: 29127662]
  • Sheikh Fayaz Ahmad, Khairy M A Zoheir, Mushtaq Ahmad Ansari, Ahmed Nadeem, Saleh A Bakheet, Ali R Al-Hoshani, Othman A Al-Shabanah, Mohammed M Al-Harbi, Sabry M Attia. Histamine 4 receptor promotes expression of costimulatory B7.1/B7.2 molecules, CD28 signaling and cytokine production in stress-induced immune responses. Journal of neuroimmunology. 2015 Dec; 289(?):30-42. doi: 10.1016/j.jneuroim.2015.10.008. [PMID: 26616869]
  • Eleonora Veglia, Cristina Grange, Alessandro Pini, Aldo Moggio, Cecilia Lanzi, Giovanni Camussi, Paul L Chazot, Arianna Carolina Rosa. Histamine receptor expression in human renal tubules: a comparative pharmacological evaluation. Inflammation research : official journal of the European Histamine Research Society ... [et al.]. 2015 Apr; 64(3-4):261-70. doi: 10.1007/s00011-015-0807-z. [PMID: 25725698]
  • Adel R A Abd-Allah, Sheikh Fayaz Ahmad, Ibrahim Alrashidi, Hala E Abdel-Hamied, Khairy M A Zoheir, Abdelkader E Ashour, Saleh A Bakheet, Sabry M Attia. Involvement of histamine 4 receptor in the pathogenesis and progression of rheumatoid arthritis. International immunology. 2014 Jun; 26(6):325-40. doi: 10.1093/intimm/dxt075. [PMID: 24402309]
  • Detlef Neumann, Silke Beermann, Heike Burhenne, Silke Glage, Christina Hartwig, Roland Seifert. The dual H3/4R antagonist thioperamide does not fully mimic the effects of the 'standard' H4R antagonist JNJ 7777120 in experimental murine asthma. Naunyn-Schmiedeberg's archives of pharmacology. 2013 Nov; 386(11):983-90. doi: 10.1007/s00210-013-0898-4. [PMID: 23820873]
  • 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]
  • Silke Beermann, Silke Glage, Danny Jonigk, Roland Seifert, Detlef Neumann. Opposite effects of mepyramine on JNJ 7777120-induced amelioration of experimentally induced asthma in mice in sensitization and provocation. PloS one. 2012; 7(1):e30285. doi: 10.1371/journal.pone.0030285. [PMID: 22272324]
  • Eriko Suwa, Katsunori Yamaura, Manabu Oda, Takao Namiki, Koichi Ueno. Histamine H(4) receptor antagonist reduces dermal inflammation and pruritus in a hapten-induced experimental model. European journal of pharmacology. 2011 Sep; 667(1-3):383-8. doi: 10.1016/j.ejphar.2011.05.037. [PMID: 21664903]
  • Zhi-qiang Yan, Ru-xin Zhang, Shao-qing Yu, Wu Wen, Jin-ke Hong, Jun Zhang, Xiao-li Shao, Sheng-hong Gao. [Effect of histamine H4 receptor and its antagonist on allergic rhinitis in rats]. Zhonghua er bi yan hou tou jing wai ke za zhi = Chinese journal of otorhinolaryngology head and neck surgery. 2010 Jun; 45(6):477-80. doi: NULL. [PMID: 21055325]
  • Herman D Lim, Chris de Graaf, Wen Jiang, Payman Sadek, Patricia M McGovern, Enade P Istyastono, Remko A Bakker, Iwan J P de Esch, Robin L Thurmond, Rob Leurs. Molecular determinants of ligand binding to H4R species variants. Molecular pharmacology. 2010 May; 77(5):734-43. doi: 10.1124/mol.109.063040. [PMID: 20103609]
  • Tadashi Kohyama, Yasuhiro Yamauchi, Hajime Takizawa, Sumiko Kamitani, Shin Kawasaki, Takahide Nagase. Histamine stimulates human lung fibroblast migration. Molecular and cellular biochemistry. 2010 Apr; 337(1-2):77-81. doi: 10.1007/s11010-009-0287-y. [PMID: 19851834]
  • Yuji Takahashi, Yoto Kagawa, Kana Izawa, Rie Ono, Masaaki Akagi, Chiaki Kamei. Effect of histamine H4 receptor antagonist on allergic rhinitis in mice. International immunopharmacology. 2009 Jun; 9(6):734-8. doi: 10.1016/j.intimp.2009.02.011. [PMID: 19275949]
  • L G Morin. Improved separation of creatine kinase cardiac isoenzyme in serum by batch fractionation. Clinical chemistry. 1976 Jan; 22(1):92-7. doi: NULL. [PMID: 1160]