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CAS No. : 459168-41-3
MCE 国际站:JNJ-7777120
产品活性:JNJ-7777120是一种强效的和具有选择性的 组胺 H4 受体 拮抗剂 (Ki=4.5 nM)。JNJ-7777120 能有效阻断组胺诱导的小鼠气管肥大细胞从结缔组织向上皮细胞的迁移。JNJ-7777120 还能在小鼠 Zymosan 诱导的腹膜炎模型中显著阻断中性粒细胞的浸润。JNJ-7777120 具有研究抗瘙痒和抗炎的较好潜力。
研究领域:GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation
作用靶点:Histamine Receptor
In Vitro: JNJ-7777120 (0, 10, 100, 1000 nM; ~6 h) shows functional antagonism of the human and mouse histamine H4 receptors in SK-N-MC cells.
JNJ-7777120 (10 µM; 10 min) blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells.
JNJ7777120 (30-100 µM; 30 min) inhibits dose-dependently the production of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 from antigen-stimulated BMMC.
In Vivo: JNJ-7777120 shows equipotent against the human, mouse, and rat receptors and exhibits at least 1000-fold selectivity over H1, H2, or H3 receptors.
JNJ-7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ~3 h in both species.
JNJ-7777120 (20 mg/kg; s.c.; single daily for 2 days) blocks the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice.
JNJ-7777120 (10 mg/kg; s.c.; single) significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model.
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