JNJ-7777120 - CAS 459168-41-3
Catalog number: 459168-41-3
Category: Inhibitor
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Histamine Receptor
JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
JNJ7777120; JNJ-7777120; JNJ 7777120.
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1.The modulatory role of spinally located histamine receptors in the regulation of the blood glucose level in d-glucose-fed mice.
Sim YB1, Park SH1, Kim SS1, Kim CH1, Kim SJ1, Lim SM1, Jung JS1, Ryu OH2, Choi MG2, Suh HW1. Korean J Physiol Pharmacol. 2014 Feb;18(1):41-6. doi: 10.4196/kjpp.2014.18.1.41. Epub 2014 Feb 13.
The possible roles of spinal histamine receptors in the regulation of the blood glucose level were studied in ICR mice. Mice were intrathecally (i.t.) treated with histamine 1 (H1) receptor agonist (2-pyridylethylamine) or antagonist (cetirizine), histamine 2 (H2) receptor agonist (dimaprit) or antagonist (ranitidine), histamine 3 (H3) receptor agonist (α-methylhistamine) or antagonist (carcinine) and histamine 4 (H4) receptor agonist (VUF 8430) or antagonist (JNJ 7777120), and the blood glucose level was measured at 30, 60 and 120 min after i.t. administration. The i.t. injection with α-methylhistamine, but not carcinine slightly caused an elevation of the blood glucose level. In addition, histamine H1, H2, and H4 receptor agonists and antagonists did not affect the blood glucose level. In D-glucose-fed model, i.t. pretreatment with cetirizine enhanced the blood glucose level, whereas 2-pyridylethylamine did not affect. The i.t. pretreatment with dimaprit, but not ranitidine, enhanced the blood glucose level in D-glucose-fed model.
2.The histamine H4 receptor is a potent inhibitor of adhesion-dependent degranulation in human neutrophils.
Dib K1, Perecko T2, Jenei V3, McFarlane C4, Comer D4, Brown V4, Katebe M5, Scheithauer T4, Thurmond RL6, Chazot PL5, Ennis M4. J Leukoc Biol. 2014 Sep;96(3):411-8. doi: 10.1189/jlb.2AB0813-432RR. Epub 2014 May 5.
The histamine H4 receptor regulates the inflammatory response. However, it is not known whether this receptor has a functional role in human neutrophils. We found that fMLP (1 μM), but not histamine (0.1-1 μM), induced Mac-1-dependent adhesion, polarization, and degranulation (release of lactoferrin). A pretreatment of neutrophils with histamine (0.001-1 μM) or JNJ 28610244 (0.1-10 μM), a specific H4 receptor agonist, led to inhibition of degranulation. Total inhibition of degranulation was obtained with 0.1 μM histamine and 10 μM JNJ 28610244. Furthermore, such inhibition by histamine of degranulation was reversed by JNJ 7777120 and JNJ 28307474, two selective H4 receptor antagonists. However, neither histamine nor the H4 receptor agonist JNJ 28610244 prevented fMLP-induced, Mac-1-dependent adhesion, indicating that the H4 receptor may block signals emanating from Mac-1-controlling degranulation. Likewise, engagement of the H4 receptor by the selective agonist JNJ 28610244 blocked Mac-1-dependent activation of p38 MAPK, the kinase that controls neutrophil degranulation.
3.Histamine H4 and H1 receptors contribute to postinflammatory visceral hypersensitivity.
Deiteren A1, De Man JG1, Ruyssers NE1, Moreels TG2, Pelckmans PA2, De Winter BY1. Gut. 2014 Dec;63(12):1873-82. doi: 10.1136/gutjnl-2013-305870. Epub 2014 Feb 21.
OBJECTIVES: Substantial evidence implicates mast cells and their main constituent histamine in the pathogenesis of visceral hypersensitivity. We explored the specific contribution of histamine H4 (H4R) and H1 (H1R) receptors to visceral hypersensitivity in a postinflammatory rat model.
4.Histamine 4 receptor promotes expression of costimulatory B7.1/B7.2 molecules, CD28 signaling and cytokine production in stress-induced immune responses.
Ahmad SF1, Zoheir KM2, Ansari MA3, Nadeem A3, Bakheet SA3, Al-Hoshani AR3, Al-Shabanah OA3, Al-Harbi MM3, Attia SM4. J Neuroimmunol. 2015 Dec 15;289:30-42. doi: 10.1016/j.jneuroim.2015.10.008. Epub 2015 Oct 22.
Recently, the expression of histamine 4 receptor (H4R) on neurons was reported, however its function in cells within the central nervous system (CNS) remains poorly understood. To this end, we used the H4R agonist, 4-methylhistamine (4-MeH), and the H4R antagonist, JNJ77777120 (JNJ), to investigate the function of H4R signaling in immune cells in a murine model of chronic stress. Treatment of stressed mice with 4-MeH resulted in an increase in the proportion of lymphocyte subsets (CD3(+), CD8(+), CD28(+), and CD4(+)CD28(+)) and cells expressing the co-stimulatory molecules CD80(+) (B7.1) and CD86(+) (B7.2) in heparinized blood as compared to normal control (NC) and stressed control (SC) groups. We also observed that as compared to NC and SC mice, 4-MeH-treated mice showed greater production of IL-2(+), IL-6(+), IL-9(+), IL-21(+), and IL-27(+) cytokines in the spleen and by splenic CD4(+) T cells. Furthermore, 4-MeH treatment of stressed mice led to an increase in the levels of serum Th1/Th17 cytokines and corticosterone, and a decrease in Th2 cytokines.
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CAS 459168-41-3 JNJ-7777120

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