JNJ-5207852 dihydrochloride

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JNJ-5207852 dihydrochloride is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

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JNJ-5207852 dihydrochloride Chemical Structure

CAS No. : 1782228-76-5

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5 mg	Get quote	Estimated Time of Arrival: December 31
10 mg	Get quote	Estimated Time of Arrival: December 31
50 mg	Get quote	Estimated Time of Arrival: December 31
100 mg	Get quote	Estimated Time of Arrival: December 31

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Other Forms of JNJ-5207852 dihydrochloride:

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
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Description

JNJ-5207852 dihydrochloride is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]