1-(4-(3-piperidin-1-ylpropoxy)benzyl)piperidine

Names

[ Name ]:
1-(4-(3-piperidin-1-ylpropoxy)benzyl)piperidine

[Synonym ]:
unii-4i9ovb1g7d
1-{3-[4-(1-Piperidinylmethyl)phenoxy]propyl}piperidine
Piperidine, 1-[3-[4-(1-piperidinylmethyl)phenoxy]propyl]-
1-(4-(3-piperidin-1-ylpropoxy)benzyl)piperidine
1-{3-[4-(piperidin-1-ylmethyl)phenoxy]propyl}piperidine

Biological Activity

[Description]:

JNJ-5207852 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]:

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

[Target]

H3 receptor:8.9 (pKi, for rat)

H3 receptor:9.24 (pKi, for human)

[In Vivo]

In mice and rats, 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. No rebound hypersomnolence, as measured by slow-wave delta power, is observed. 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, possibly due to the compound being a neutral antagonist at the H3 receptor. JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels[1].

[Animal admin]

Rats[1] Male, Sprague-Dawley rats weighing 282-334 g are used. The animals are individually housed with free access to food and water. To assure that there are no pre-existing group differences in activity levels prior to the initiation of treatment, LMA is monitored and recorded during a 2 h habituation period. Following the 2 h habituation period, testing is briefly interrupted and animals are s.c. injected with either saline (1 mL/kg; n=6), JNJ-5207852 (3, 10, 30 mg/kg; n=6-7 animals/group) or Damphetamine (0.75 mg/kg; n=6). Testing is immediately resumed following the compound injection[1].

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.0±0.1 g/cm3

[ Boiling Point ]:
443.4±30.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₀H₃₂N₂O

[ Molecular Weight ]:
316.481

[ Flash Point ]:
123.9±21.8 °C

[ Exact Mass ]:
316.251465

[ PSA ]:
15.71000

[ LogP ]:
4.11

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.542

[ Storage condition ]:
2-8℃

1-(4-(3-piperidin-1-ylpropoxy)benzyl)piperidine

Names

Biological Activity

Chemical & Physical Properties

Related Compounds