| Identification | Back Directory | [Name]
N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide | [CAS]
1052147-86-0 | [Synonyms]
LP21
LP-211
LP-211 >=98% (HPLC)
LP-211; LP 211; LP211;1052147-86-0
N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide | [Molecular Formula]
C30H34N4O | [MDL Number]
MFCD22690843 | [MOL File]
1052147-86-0.mol | [Molecular Weight]
466.62 |
| Chemical Properties | Back Directory | [Boiling point ]
714.8±60.0 °C(Predicted) | [density ]
1.17±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);214.3(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);107.15(Max Conc. mM) | [form ]
solid | [pka]
15.39±0.46(Predicted) | [color ]
clear white to light brown |
| Hazard Information | Back Directory | [Uses]
LP-211 is a brain penetrant selective agonist for the serotonin 5-HT7 receptor used in pharmacological studies which showed that it underwent metabolic breakdown to RA-7 and showed pharmacological activities such as induced hypothermia in mice and showed optimal pharmacokinetics in rats.LP-211 is also a drug analogue of piperazinehexanamide exhibiting 5-HT7 receptor affinity. | [Biochem/physiol Actions]
LP-211 is a brain penetrant selective agonist for the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor. The 5-HT7 receptor is involved in a variety of central nervous system functions including circadian rhythm, sleep, thermoregulation, nociception, and memory, and appears to be involved in cognitive disorders, anxiety, and depression. LP-211 has been used as a selective 5-HT7 receptor agonist in multiple models including studies as a potential therapeutic agent in models of Rett syndrome and Fragile X Syndrome. | [in vivo]
LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean Cmax of 0.76 ± 0.32 μg/mL at 30 min[1]. LP-211 (0.003-0.3 mg/kg, i.p.) significantly increases the micturition volume in a dose-dependent manner, and causes significant increases in voiding efficiency in spinal cord-injured (SCI) rats, and such effects can be completely reversed by SB-269970[2]. LP-211 (0.25 and 0.50 mg/kg i.p.) improves consolidation of chamber-shape memory in rats, resulting in significant novelty-induced hyperactivity and recognition[3]. | [IC 50]
5-HT7 Receptor: 0.58 nM (Ki); 5-HT1A Receptor: 188 nM (Ki); D2 Receptor: 142 nM (Ki) | [storage]
Store at -20°C |
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
|