JNJ-7777120
JNJ-7777120 structure
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Common Name | JNJ-7777120 | ||
|---|---|---|---|---|
| CAS Number | 459168-41-3 | Molecular Weight | 277.749 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 477.0±45.0 °C at 760 mmHg | |
| Molecular Formula | C14H16ClN3O | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 242.3±28.7 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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Involvement of the H1 Histamine Receptor, p38 MAP Kinase, Myosin Light Chains Kinase, and Rho/ROCK in Histamine-Induced Endothelial Barrier Dysfunction.
Microcirculation 22 , 237-48, (2015) The mechanisms by which histamine increases microvascular permeability remain poorly understood. We tested the hypothesis that H1 receptor activation disrupts the endothelial barrier and investigated potential downstream signals.We used confluent EC monolayer... |
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Histamine H4 receptor as a new therapeutic target for choroidal neovascularization in age-related macular degeneration.
Br. J. Pharmacol. 171(15) , 3754-63, (2014) The present treatment for choroidal neovascularization (CNV) associated with age-related macular degeneration (AMD) is not sufficient. Hence, we examined the therapeutic efficacy of reducing histamine H4 receptor expression on CNV in mice.H4 receptor expressi... |
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Analysis of the histamine H2-receptor in human monocytes.
Biochem. Pharmacol. 92(2) , 369-79, (2014) Histamine receptors are G-protein-coupled receptors (GPCRs). Canonically, the histamine H2-receptor (H2R) couples to Gs-proteins and activates adenylyl cyclases (ACs) with subsequent adenosine-3',5'-cyclic monophosphate (cAMP) generation. Recently, the classi... |
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The first potent and selective non-imidazole human histamine H4 receptor antagonists.
J. Med. Chem. 46 , 3957-3960, (2003) 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 t... |
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Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines.
Respir. Res. 11 , 86, (2010) Airway remodeling and dysfunction are characteristic features of asthma thought to be caused by aberrant production of Th2 cytokines. Histamine H4 receptor (H4R) perturbation has previously been shown to modify acute inflammation and Th2 cytokine production i... |
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Ligand Residence Time at G-protein-Coupled Receptors-Why We Should Take Our Time To Study It.
Mol. Pharmacol. 88 , 552-60, (2015) Over the past decade the kinetics of ligand binding to a receptor have received increasing interest. The concept of drug-target residence time is becoming an invaluable parameter for drug optimization. It holds great promise for drug development, and its opti... |
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Inhibition of histamine-mediated signaling confers significant protection against severe malaria in mouse models of disease.
J. Exp. Med. 205 , 395-408, (2008) From the inoculation of Plasmodium sporozoites via Anopheles mosquito bites to the development of blood-stage parasites, a hallmark of the host response is an inflammatory reaction characterized by elevated histamine levels in the serum and tissues. Given the... |
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The histamine h4 receptor regulates chemokine production in human natural killer cells.
Int. Arch. Allergy Immunol. 166 , 225-30, (2015) Natural killer (NK) cells have been detected in the lesional skin of patients with inflammatory skin diseases, where high levels of histamine are also present. Therefore, we investigated the effect of histamine, in particular via the histamine H4 receptor (H4... |