1782228-76-5

1782228-76-5 structure
1782228-76-5 structure
  • Name: JNJ 5207852 dihydrochloride
  • Chemical Name: JNJ-5207852 dihydrochloride
  • CAS Number: 1782228-76-5
  • Molecular Formula: C20H34Cl2N2O
  • Molecular Weight: 389.40
  • Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
  • Create Date: 2020-08-11 17:45:06
  • Modify Date: 2024-01-09 22:13:03
  • JNJ-5207852 dihydrochloride is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.

Name JNJ-5207852 dihydrochloride
Description JNJ-5207852 dihydrochloride is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
Related Catalog
Target

H3 Receptor:8.9 (pKi, for rat)

H3 Receptor:9.24 (pKi, for human)

In Vivo 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[1]. Animal Model: Male, Sprague-Dawley rats weighing 282-334 g[1]. Dosage: 3, 10, 30 mg/kg. Administration: S.C. Result: Iincreased time spent awake and decreased REM sleep and slow-wave sleep.
References

[1]. Barbier AJ, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.

[2]. Abuhamdah RM, et al. Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze. Front Syst Neurosci. 2012 Jul 16;6:54.

Molecular Formula C20H34Cl2N2O
Molecular Weight 389.40
Hazard Codes Xn