459168-41-3 Usage
Description
JNJ7777120 is a histamine 4 receptor (H4R) antagonist that has been utilized in various research studies to understand its effects on different biological processes and conditions. It is known for its ability to inhibit the production of certain chemokines, which are small proteins involved in immune responses and inflammation.
Uses
Used in Pharmaceutical Research:
JNJ7777120 is used as a histamine-4 receptor antagonist for studying its effects on various biological processes and conditions. It has been employed in the following applications:
1. Atopic Dermatitis Treatment:
JNJ7777120 is used as a therapeutic agent for atopic dermatitis, a chronic inflammatory skin condition. It works by inhibiting the production of CCL17 and CCL22 chemokines by human monocyte-derived Langerhans cells, which play a role in the pathogenesis of the disease.
2. Neuroinflammation and Microglial Activation:
JNJ7777120 is used as a research tool to study its effects on pro-inflammatory microglia in rats. Microglia are immune cells in the central nervous system that can become activated in response to injury or disease, leading to inflammation and potentially contributing to neurodegenerative conditions.
3. Parkinson's Disease Research:
JNJ7777120 is used as a histamine-4 receptor antagonist to study its effects on Parkinson's-like pathology in rat brain models. This research aims to understand the role of histamine receptors in the development and progression of Parkinson's disease, a neurodegenerative disorder characterized by the loss of dopaminergic neurons and the presence of Lewy bodies.
4. Periodontal Ligament Fibroblasts (PDLF) Research:
JNJ7777120 is used as a histamine receptor antagonist to study its effects on the interaction between histamine receptors and periodontal ligament fibroblasts. This research could provide insights into the role of histamine receptors in periodontal health and disease, potentially leading to new therapeutic approaches for periodontal conditions.
Biological Activity
histamine has been reported to play an important role in a large number of physiological processes. jnj-7777120, the first potent and selective non-imidazole histamine h4 receptor antagonist with ki of 4.5 nm, exhibits more than 1000-fold selectivity over the other histamine receptors. [1]
Biochem/physiol Actions
JNJ7777120 may exhibit neuroprotective effects against ischemic brain damage. It acts as an anti-inflammatory agent to treat inflammatory diseases. JNJ7777120 is observed to reduce colonic injury, cytokine production, and neutrophil infiltration.
in vitro
it was reported that nj 7777120 bound to the h4 receptor with a remarkably high affinity. it also demonstrated a greater selectivity over other histamine receptor antagonists. moreover, jnj 7777120 selectively targeted to potent h4 rather than 50 other molecular targets. [2]
in vivo
jnj 7777120 showed an oral bioavailability of about 30% in rats and 100% in dogs, with a half-life of around 3 h in both rats and dogs. it was reported to inhibit histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. in addition, in mice, jnj 7777120 could suppress the histamine-induced migration of tracheal mast cells from the connective tissue to the epithelium. moreover, jnj 7777120 was demonstrated to notably inhibit neutrophil infiltration in a mouse zymosan-induced peritonitis model. [2]
IC 50
a histamine h4 receptor antagonist with ic50 of 4.5 nm.
references
[1]jablonowski ja, grice ca, chai w, dvorak ca, venable jd, kwok ak, ly ks, wei j, baker sm, desai pj, jiang w, wilson sj, thurmond rl, karlsson l, edwards jp, lovenberg tw and carruthers ni. the first potent and selective non-imidazole human histamine h4 receptor antagonists. j med chem. 2003 sep; 46(19): 3957-60.[2]thurmond rl, desai pj, dunford pj, fung-leung wp, hofstra cl, jiang w, nguyen s, riley jp, sun s, williams kn, edwards jp and karlsson l. a potent and selective histamine h4 receptor antagonist with anti-inflammatory properties. j pharmacol exp ther. 2004 apr; 309(1): 404-13.
Check Digit Verification of cas no
The CAS Registry Mumber 459168-41-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,5,9,1,6 and 8 respectively; the second part has 2 digits, 4 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 459168-41:
(8*4)+(7*5)+(6*9)+(5*1)+(4*6)+(3*8)+(2*4)+(1*1)=183
183 % 10 = 3
So 459168-41-3 is a valid CAS Registry Number.
InChI:InChI=1/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3