1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. JNJ-5207852 dihydrochloride

JNJ-5207852 dihydrochloride 

Cat. No.: HY-12190A
Handling Instructions

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.

For research use only. We do not sell to patients.

JNJ-5207852 dihydrochloride Chemical Structure

JNJ-5207852 dihydrochloride Chemical Structure

CAS No. : 1782228-76-5

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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.

IC50 & Target[1]

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.
Molecular Weight

389.40

Formula

C₂₀H₃₄Cl₂N₂O

CAS No.

1782228-76-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

JNJ-5207852JNJ5207852JNJ 5207852Histamine ReceptorlowtoxicityREMsleepInhibitorinhibitorinhibit

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JNJ-5207852 dihydrochloride
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HY-12190A
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