Literature DB >> 12954048

The first potent and selective non-imidazole human histamine H4 receptor antagonists.

Jill A Jablonowski1, Cheryl A Grice, Wenying Chai, Curt A Dvorak, Jennifer D Venable, Annette K Kwok, Kiev S Ly, Jianmei Wei, Sherry M Baker, Pragnya J Desai, Wen Jiang, Sandy J Wilson, Robin L Thurmond, Lars Karlsson, James P Edwards, Timothy W Lovenberg, Nicholas I Carruthers.   

Abstract

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.

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Year:  2003        PMID: 12954048     DOI: 10.1021/jm0341047

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  36 in total

Review 1.  Histamine H4 antagonism: a therapy for chronic allergy?

Authors:  Bruce L Daugherty
Journal:  Br J Pharmacol       Date:  2004-05       Impact factor: 8.739

Review 2.  Molecular and biochemical pharmacology of the histamine H4 receptor.

Authors:  Rob Leurs; Paul L Chazot; Fiona C Shenton; Herman D Lim; Iwan J P de Esch
Journal:  Br J Pharmacol       Date:  2009-05       Impact factor: 8.739

Review 3.  The role of histamine H4 receptor in immune and inflammatory disorders.

Authors:  E Zampeli; E Tiligada
Journal:  Br J Pharmacol       Date:  2009-03-20       Impact factor: 8.739

4.  Studies of H4R antagonists using 3D-QSAR, molecular docking and molecular dynamics.

Authors:  Jing Liu; Yan Li; Hui-Xiao Zhang; Shu-Wei Zhang; Ling Yang
Journal:  J Mol Model       Date:  2011-06-07       Impact factor: 1.810

5.  Chemical structural novelty: on-targets and off-targets.

Authors:  Emmanuel R Yera; Ann E Cleves; Ajay N Jain
Journal:  J Med Chem       Date:  2011-09-14       Impact factor: 7.446

6.  Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability.

Authors:  G Desmadryl; S Gaboyard-Niay; A Brugeaud; C Travo; A Broussy; A Saleur; J Dyhrfjeld-Johnsen; E Wersinger; C Chabbert
Journal:  Br J Pharmacol       Date:  2012-10       Impact factor: 8.739

7.  The histamine H4 receptor is a potent inhibitor of adhesion-dependent degranulation in human neutrophils.

Authors:  Karim Dib; Tomas Perecko; Veronika Jenei; Cheryl McFarlane; David Comer; Vanessa Brown; Mwape Katebe; Torsten Scheithauer; Robin L Thurmond; Paul L Chazot; Madeleine Ennis
Journal:  J Leukoc Biol       Date:  2014-05-05       Impact factor: 4.962

8.  A search for functional histamine H4 receptors in the human, guinea pig and mouse brain.

Authors:  Monika Feliszek; Valerie Speckmann; Daniel Schacht; Marec von Lehe; Holger Stark; Eberhard Schlicker
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2014-10-10       Impact factor: 3.000

9.  Role of a histamine 4 receptor as an anti-inflammatory target in carrageenan-induced pleurisy in mice.

Authors:  Sheikh Fayaz Ahmad; Khairy M A Zoheir; Hala E Abdel-Hamied; Ibrahim Alrashidi; Sabry M Attia; Saleh A Bakheet; Abdelkader E Ashour; Adel R A Abd-Allah
Journal:  Immunology       Date:  2014-07       Impact factor: 7.397

10.  Postsynaptic mechanisms underlying the excitatory action of histamine on medial vestibular nucleus neurons in rats.

Authors:  Xiao-Yang Zhang; Lei Yu; Qian-Xing Zhuang; Shi-Yu Peng; Jing-Ning Zhu; Jian-Jun Wang
Journal:  Br J Pharmacol       Date:  2013-09       Impact factor: 8.739

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