Selective, non-imidazole histamine H3R antagonist
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JNJ-5207852

Item No. 11998

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[3-[4-(1-piperidinylmethyl)phenoxy]propyl]-piperidine
CAS Number
398473-34-2
Molecular Formula
C20H32N2O
Formula Weight
316.5
Purity
≥98%
Formulation
A 10 mg/ml solution in ethanol
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 5 mg/mlEthanol: 16 mg/mlPBS (pH 7.2): 0.25 mg/ml
λmax
226, 275 nm
SMILES
N1(CC2=CC=C(OCCCN3CCCCC3)C=C2)CCCCC1
InChi Code
InChI=1S/C20H32N2O/c1-3-12-21(13-4-1)16-7-17-23-20-10-8-19(9-11-20)18-22-14-5-2-6-15-22/h8-11H,1-7,12-18H2
InChi Key
PTKHFRNHJULJKT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $98

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    10 mg

    $185

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    50 mg

    $770

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    Product Description

    Histamine has been implicated in a variety of biological functions including thermo- and immunoregulation, food intake, hyperexcitability, pain transmission, arousal, reward, memory, and emotional responses. The histamine H3 receptor is a Gi-coupled presynaptic auto- and hetero-receptor whose activation leads to a decreased release of histamine, glutamate, norepinephrine, and acetylcholine in the brain. H3R antagonists are expected to increase the release of these neurotransmitters, which may contribute therapeutic benefit in diseases characterized by sleep/wake disturbances or cognitive disorders.1,2 JNJ-5207852 is a selective, non-imidazole histamine H3R antagonist with high affinity at the rat (pKi = 8.9) and human (pKi = 9.24) H3 receptors.3 In rodents, 1-10 mg/kg JNJ-5207852 administered subcutaneously increases time spent awake and decreases REM sleep and slow-wave sleep.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tiligada, E., Zampeli, E., Sander, K., et al. Histamine H3 and H4 receptors as novel drug targets. Expert. Opin. Investig. Drugs 18(10), 1519-1532 (2009).

    2. Barbier, A.J., Dugovic, B.C., Laposky, A.D., et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br. J. Pharmacol. 143(5), 649-661 (2004).

    3. Esbenshade, T.A., Browman, K.E., Bitner, R.S., et al. The histamine H3 receptor: An attractive target for the treatment of cognitive disorders. Br. J. Pharmacol. 154(6), 1166-1181 (2008).