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JNJ-39758979 dihydrochloride
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JNJ-39758979 dihydrochloride
CAS No. :
MCE 站:JNJ-39758979 dihydrochloride
产品活性:JNJ-39758979 dihydrochloride 是一种选择性的、具有口服活性的、高亲和力的组胺 H4 受体 (histamine H4 receptor) 拮抗剂,对人,小鼠,猴子的组胺 H4 受体的 Ki 值分别为12.5、5.3 和 25 nM。JNJ-39758979 dihydrochloride 对组胺诱导的 cAMP 抑制作用具有拮抗作用,pA2 为 7.9。JNJ-39758979 dihydrochloride 具有良好的抗炎、止痒作用。
研究领域:GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation
作用靶点:Histamine Receptor
In Vitro: JNJ-39758979 dihydrochloride is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM versus the human H4 receptor and functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. At the mouse H4R, the Ki=5.3 nM and the pA2=8.3. At the monkey H4R, the Ki=25 nM and the pA2=7.5. The affinity for the rat (Ki=188 nM, pA2 = 7.2) and guinea pig H4R (Ki=306 nM) is moderate, and JNJ-39758979 dihydrochloride has little if any affinity for the dog H4R (Ki≥10 μM). The compound is highly selective for H4R, as it exhibits low affinity for the H1, H2, and H3 receptors.
JNJ-39758979 dihydrochloride is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes.
In Vivo: JNJ-39758979 dihydrochloride (10 mg/kg; p.o.) treatment shows that the Cmax, t1/2 and F values are 0.3 μM, 7.5 hours, 36%, respectively.
JNJ-39758979 dihydrochloride (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t1/2 were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively .
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