JNJ-5207852

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 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.

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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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398473-34-2

316.48

C20H32N2O

>98% (HPLC)

DMSO:77.5 mg/mL (244.88 mM)

C(COc1ccc(CN2CCCCC2)cc1)CN1CCCCC1

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(-20℃)

With Ice Pack

≥ 2 years