JNJ-5207852 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ-5207852 是一种新型非咪唑组胺 H3 受体拮抗剂，对大鼠 (pKi=8.9) 和人 (pKi=9.24) H3 受体具有高亲和力。 JNJ-5207852 是一种有效的二元胺拮抗剂，可有效结合大鼠 H3 受体 (Ki=1.2nm），具有良好的脑穿透力。在小鼠离体结合研究中，该化合物的 ED50 为 0.13毫克公斤-1、皮下注射。

JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor. JNJ-5207852 is a potent dibasic amine antagonist that binds potently to rat H3 receptors (Ki=1.2?nm), and has good brain penetration. In ex vivo binding studies in mice, the compound had an ED50 of 0.13?mg?kg?1, subcutaneously. It promotes wakefulness in rodents at 10?mg?kg?1 s.c. but not at 1?mg?kg?1, and significantly, this effect was absent in H3 receptor KO mice. JNJ-10181457 is also a dibasic amine antagonist that exhibits high-affinity binding for the rat H3 receptor (Ki=7.1?nm), promoting wakefulness in rodents and reducing cataplectic attacks in narcoleptic dogs . JNJ-10181457 improved cognitive performance in SHR pups at 10?mg?kg?1.

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JNJ-5207852 (1-10mg/kg s.c.) increases time spent awake and decreases REM sleep and slow-wave sleep, but fails to have an effect on wakefulness or sleep in H3 receptor knockout mice. The wake promoting effects of this H3 receptor antagonist are not associated with hypermotility. A 4-week daily treatment of mice with JNJ-5207852 (10 mg/kg i.p.) does not lead to a change in body weight. JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels. Animal Model:Male, Sprague-Dawley ratsweighing 282-334 g.Dosage:3, 10, 30 mg/kg.Administration:S.C. Result:Iincreased time spent awake and decreased REM sleep and slow-wave sleep.

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GPCR/G Protein

Histamine Receptor

H3 receptor

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1782228-76-5

389.4

C20H34Cl2N2O?

>98% (HPLC)

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[H]Cl.[H]Cl.N1(CCCOC2=CC=C(CN3CCCCC3)C=C2)CCCCC1

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(-20℃)

With Ice Pack

≥ 2 years