398473-34-2
398473-34-2 structure
- Name: 1-(4-(3-piperidin-1-ylpropoxy)benzyl)piperidine
- Chemical Name: 1-[3-[4-(piperidin-1-ylmethyl)phenoxy]propyl]piperidine
- CAS Number: 398473-34-2
- Molecular Formula: C20H32N2O
- Molecular Weight: 316.481
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2016-03-21 19:37:00
- Modify Date: 2024-01-06 12:45:57
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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.
| Name | 1-[3-[4-(piperidin-1-ylmethyl)phenoxy]propyl]piperidine |
|---|---|
| Synonyms |
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 |
| 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 | |
| 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 |
| 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℃ |