Journal of Medicinal Chemistry 2003-09-11

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

Jill A Jablonowski, 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

Index: J. Med. Chem. 46 , 3957-3960, (2003)

Full Text: HTML

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.

Related Compounds

  • JNJ-7777120
  • 5-Methyl-1H-indol...

Related Articles:

Involvement of the H1 Histamine Receptor, p38 MAP Kinase, Myosin Light Chains Kinase, and Rho/ROCK in Histamine-Induced Endothelial Barrier Dysfunction.

2015-05-01

[Microcirculation 22 , 237-48, (2015)]

Histamine H4 receptor as a new therapeutic target for choroidal neovascularization in age-related macular degeneration.

2014-08-01

[Br. J. Pharmacol. 171(15) , 3754-63, (2014)]

Analysis of the histamine H2-receptor in human monocytes.

2014-11-15

[Biochem. Pharmacol. 92(2) , 369-79, (2014)]

Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines.

2010-01-01

[Respir. Res. 11 , 86, (2010)]

Ligand Residence Time at G-protein-Coupled Receptors-Why We Should Take Our Time To Study It.

2015-09-01

[Mol. Pharmacol. 88 , 552-60, (2015)]

More Articles...