JNJ-39758979,1046447-90-8

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JNJ-39758979

CAS No. : 1046447-90-8

MCE 国际站：JNJ-39758979

产品活性：JNJ-39758979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 K_i 值分别为 12.5、5.3 和 25 nM。JNJ-39758979 对组胺诱导的 cAMP 抑制作用具有拮抗作用，pA2 为 7.9。JNJ-39758979 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 is a selective, high-affinity histamine H₄ receptor antagonist with a K_i 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 K_i=5.3 nM and the pA2=8.3. At the monkey H₄R, the K_i=25 nM and the pA2=7.5. The affinity for the rat (K_i=188 nM, pA2 = 7.2) and guinea pig H₄R (K_i=306 nM) is moderate, and JNJ 39758979 has little if any affinity for the dog H₄R (K_i≥10 μM). The compound is highly selective for H₄R, as it exhibits low affinity for the H₁, H₂, and H₃ receptors.
JNJ-39758979 is metabolically stable (t_1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes.

In Vivo: JNJ-39758979 (10 mg/kg; p.o.) treatment shows that the C_max, t_1/2 and F values are 0.3 μM, 7.5 hours, and 36%, respectively.
JNJ-39758979 (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t_1/2 were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively .

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