JNJ 10191584 maleate
Chemical Name: 1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazine maleate
Biological ActivityJNJ 10191584 maleate is a highly selective histamine H4 receptor silent antagonist; binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM). Inhibits mast cell and eosinophil chemotaxis in vitro with IC50 values of 138 and 530 nM respectively. Orally active in vivo.
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Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists.
Terzioglu et al.
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H4 antagonists.
Venable et al.
Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.
Varga et al.
Citations for JNJ 10191584 maleate
The citations listed below are publications that use Tocris products. Selected citations for JNJ 10191584 maleate include:
3 Citations: Showing 1 - 3
Histamine H3 receptor antagonist OUP-186 attenuates the proliferation of cultured human breast cancer cell lines
Authors: Tanaka Et al.
Biochemical and Biophysical Research Communication 2016;480:479
Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability.
Authors: Desmadryl Et al.
Br J Pharmacol 2012;167:905
The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS.
Authors: Connelly Et al.
Br J Pharmacol 2009;157:55
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