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KI1110JNJ-5207852QuoteQuote

Chemical Characteristic

Product NameJNJ-5207852
CAS No.398473-34-2
Molecular Weight 316.48
FormulaC20H32N2O
Chemical Name1-[3-[4-(piperidin-1-ylmethyl)phenoxy]propyl]piperidine
SmilesN1(CCCCC1)CCCOc1ccc(cc1)CN1CCCCC1
Chemical Structure

Biological activities

JNJ-5207852 is a selective histamine H3 subtype antagonist. The pKi of JNJ-5207852 is 8.9 and 9.24 against rat and human H3 receptors. JNJ-5207852 fails to bind to human H1, H2 or H4 histamine receptors. JNJ-5207852 readily penetrates the brain tissue after subcutaneous (s.c.) administration with an ED50 of 0.13 mg/kg.[1] JNJ-5207852 ameliorates pentylenetetrazol kindling-induced learning and mnemonic deficits.[2] In mice and rats, JNJ-5207852 ranging from 1 to 10 mg/kg subcutaneously increases time spent awake and decreases REM sleep and slow-wave sleep, but does not have an effect on wakefulness or sleep in H3 receptor knockout mice. Administration of JNJ-5207852 (10 mg/kg) significantly increases wakefulness in H3+/+ mice. JNJ-5207852 also increases the amount of wakefulness and decreases SWS time in mice. [1]

Protocols

In vivo JNJ-5207852 is dissolved in saline.[1]

References

[1] Barbier AJ, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004, 143(5): 649-661.
[2] Jia F, et al. Effects of histamine H(3) antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice. Neuropharmacology. 2006, 50(4): 404-411.

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