JNJ-39758979 dihydrochloride 是一种选择性、口服活性、高亲和力的组胺 H4受体拮抗剂 (histamine H4 receptor)，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 对转染细胞中组胺诱导的 cAMP 抑制作用具有拮抗作用，pA2 为 7.9。JNJ-39758979 dihydrochloride 具有良好的抗炎和止痒活性。

JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist for human, mouse, and monkey histamine H4 receptor with Ki s of 12.5, 5.3, and 25 nM, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride exhibits good anti-inflammatory and antipruritic activity [1] [2].

JNJ-39758979 dihydrochloride is a selective, high-affinity histamine H 4 receptor antagonist with a K i of 12.5 nM to the human H 4 receptor and functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. At the mouse H 4 R, the K i =5.3 nM and the pA2=8.3. At the monkey H 4 R, 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 H 4 R (K i =306 nM) is moderate, and JNJ-39758979 dihydrochloride has little if any affinity for the dog H 4 R (K i ≥10 μM). The compound is highly selective for H 4 R because it exhibits low affinity for the H 1, H 2, and H 3 receptors [1]. JNJ-39758979 dihydrochloride is metabolically stable (t 1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes [1].

Treatment with JNJ-39758979 dihydrochloride (10 mg/kg; p.o.) exhibits that the C max, t 1/2 and F values are 0.3 μM, 7.5 hours, 36%, respectively [1]. Treatment with JNJ-39758979 dihydrochloride (2 mg/kg; i.v.) exhibits 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 [1]. Animal Model: Sprague-Dawley rats [1] Dosage: 10 mg/kg Administration: Oral administration (Pharmacokinetic Analysis) Result: The C max, t 1/2 and F values were 0.3 μM, 7.5 hours, and 36%, respectively.

T11723

C11H21Cl2N5

294.22

JNJ-39758979 dihydrochloride (1046447-90-8 free base);JNJ-39758979 dihydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years