JNJ-10191584 - CAS 73903-17-0
Catalog number: 73903-17-0
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Histamine Receptor
JNJ-10191584 is a selective histamine H4 receptor antagonist. It inhibits mast cell in vitro with IC50 value of 138nM. JNJ-10191584 has antiinflammatory and analgesic effects in animal studies of acute inflammation. No development was reported for the treatment of Allergic rhinitis, Atopic dermatitis, Pruritus and Respiratory tract disorders.
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JNJ-10191584; JNJ10191584; JNJ 10191584; VUF-6002; VUF 6002; VUF6002; (5-Chloro-1H-benzimidazol-2-yl)(4-methylpiperazin-1-yl)methanone;869497-75-6(maleate)
Solubility in DMSO: ~ 19 mg/ml (or 68 mM)
-20℃ Freezer
Allergic rhinitis; Atopic dermatitis; Pruritus; Respiratory tract disorders
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Boiling Point:
No Data Available
Canonical SMILES:
Current Developer:
Janssen Research & Development
1.The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS.
Connelly WM;Shenton FC;Lethbridge N;Leurs R;Waldvogel HJ;Faull RL;Lees G;Chazot PL Br J Pharmacol. 2009 May;157(1):55-63. doi: 10.1111/j.1476-5381.2009.00227.x.
BACKGROUND AND PURPOSE: ;The histamine H4 receptor is the most recently identified of the G protein-coupled histamine receptor family and binds several neuroactive drugs, including amitriptyline and clozapine. So far, H4 receptors have been found only on haematopoietic cells, highlighting its importance in inflammatory conditions. Here we investigated the possibility that H4 receptors may be expressed in both the human and mouse CNS.;METHODS: ;Immunological and pharmacological studies were performed using a novel anti-H4 receptor antibody in both human and mouse brains, and electrophysiological techniques in the mouse brain respectively. Pharmacological tools, selective for the H4 receptor and patch clamp electrophysiology, were utilized to confirm functional properties of the H4 receptor in layer IV of the mouse somatosensory cortex.;RESULTS: ;Histamine H4 receptors were prominently expressed in distinct deep laminae, particularly layer VI, in the human cortex, and mouse thalamus, hippocampal CA4 stratum lucidum and layer IV of the cerebral cortex. In layer IV of the mouse somatosensory cortex, the H4 receptor agonist 4-methyl histamine (20 micromol x L(-1)) directly hyperpolarized neurons, an effect that was blocked by the selective H4 receptor antagonist JNJ 10191584, and promoted outwardly rectifying currents in these cells.
2.Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.
Varga C;Horvath K;Berko A;Thurmond RL;Dunford PJ;Whittle BJ Eur J Pharmacol. 2005 Oct 17;522(1-3):130-8. Epub 2005 Oct 6.
The histamine H(4) receptor is a G-protein coupled receptor with little homology to the pro-inflammatory histamine H(1) receptor, expressed on cells of the immune system with hematopoietic lineage such as eosinophils and mast cells. The effects of the recently described highly selective histamine H(4) receptor antagonists JNJ 10191584 and JNJ 7777120 have now been investigated on the acute colitis provoked by trinitrobenzene sulphonic acid over 3 days in the rat. Treatment with JNJ 10191584 (10-100 mg/kg p.o., b.i.d.) caused a dose-dependent reduction in macroscopic damage, inhibition of the TNBS-provoked elevation of both colonic myeloperoxidase and tumour necrosis factor-alpha (TNF-alpha), and a reduction in the histologically assessed increase in mucosal and submucosal thickness and neutrophil infiltration. JNJ 7777120 (100 mg/kg p.o., b.i.d.) likewise reduced the macroscopic injury and the increases in colonic myeloperoxidase and TNF-alpha levels. These findings indicate a pro-inflammatory role for the histamine H(4) receptor in this model and suggest a novel pharmacological approach to the treatment of colitis.
3.Histamine H
Sanna MD;Lucarini L;Durante M;Ghelardini C;Masini E;Galeotti N Br J Pharmacol. 2017 Jan;174(1):28-40. doi: 10.1111/bph.13644. Epub 2016 Nov 18.
BACKGROUND AND PURPOSE: ;Neuropathic pain is under-treated, with a detrimental effect on quality of life, partly because of low treatment efficacy, but also because pathophysiological mechanisms are not fully elucidated. To clarify the pathobiology of neuropathic pain, we studied the contribution of neuroinflammation and oxidative stress in a model of peripheral neuropathy. We also assessed an innovative treatment for neuropathic pain by investigating the effects of histamine H;4; receptor ligands in this model.;EXPERIMENTAL APPROACH: ;A peripheral mononeuropathy was induced in mice, by spared nerve injury (SNI). Neuroinflammation and oxidative stress parameters were evaluated by spectrophotometry. The mechanical (von Frey test) and thermal (plantar test) nociceptive thresholds were evaluated.;KEY RESULTS: ;SNI mice showed increased expression of the pro-inflammatory cytokines IL-1ß and TNF-α, decreased antioxidant enzyme Mn-containing SOD (MnSOD), increased levels of 8-hydroxy-2'-deoxyguanosine (8-OHdG), an indicator of oxidative DNA damage, and of PARP, nuclear enzyme activated upon DNA damage. Intrathecal administration of VUF 8430 (H;4; receptor agonist) reversed the mechanical and thermal allodynia and was associated with decreased expression of IL-1ß, TNF-α, 8-OHdG and PARP and with restoration of MnSOD activity in the spinal cord and sciatic nerve.
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CAS 73903-17-0 JNJ-10191584

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