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p-MPPI HCl

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Chemical Structure| 220643-77-6 同义名 : p-MPPI hydrochloride
CAS号 : 220643-77-6
货号 : A180570
分子式 : C25H28ClIN4O2
纯度 : 98+%
分子量 : 578.873
MDL号 : MFCD00467897
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(27.64 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 3 mg/mL(5.18 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 p-MPPI HCl is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. Pre-treatment with p-MPPI (5 mg/kg intraperitoneal (i.p.)) 30 min before 8-OH-DPAT (0.375 mg/kg subcutaneously (s.c.)) reduced the effect of 8-OH-DPAT on waking and REM sleep. Also, p-MPPI (5 and 10 mg/kg i.p.) reduced the effect of 8-OH-DPAT on locomotion and partially or completely antagonized hindlimb abduction and flat body posture[2]. At lower doses (0.5-4.5 mg/kg), p-MPPI produced a significant and dose-related anxiolytic profile on both conventional (open arm avoidance) and ethological (risk assessment) measures. However, these effects were lost at a higher dose (13.5 mg/kg) which, instead, increased grooming and immobility[3]. Pretreatment with p-MPPI reduced or blocked the effect of the 5-HT1A receptor agonist 8-OH-DPAT on two responses mediated by postsynaptic 5-HT1A receptors, reduction of body temperature and the 5-HT behavioral syndrome. Administration of p-MPPI alone did not alter body temperature or produce symptoms of the 5-HT syndrome. Pretreatment with p-MPPI also blocked the ability of 8-OH-DPAT to reduce extracellular 5-HT in the striatum[4]. Administration of p-MPPI at the doses of 0.4, 0.7 and 1.0 mg/kg reduced in a dose-dependent manner the ethanol-induced hypothermia and the sleep time and attenuated the ethanol-induced decrease of acoustic startle reflex magnitude in mice. Similar p-MPPI (0.4 mg/kg) effects on ethanol-induced sleep and hypothermia were obtained in rats[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.64mL

1.73mL

0.86mL

17.27mL

3.45mL

1.73mL
参考文献

[1]Cao BJ, Rodgers RJ. Anxiolytic-like profile of p-MPPI, a novel 5HT1A receptor antagonist, in the murine elevated plus-maze. Psychopharmacology (Berl). 1997;129(4):365-371. doi:10.1007/s002130050202

[2]Sørensen E, Grønli J, Bjorvatn B, Ursin R. The selective 5-HT(1A) receptor antagonist p-MPPI antagonizes sleep--waking and behavioural effects of 8-OH-DPAT in rats. Behav Brain Res. 2001 Jun;121(1-2):181-7

[3]Cao BJ, Rodgers RJ. Anxiolytic-like profile of p-MPPI, a novel 5HT1A receptor antagonist, in the murine elevated plus-maze. Psychopharmacology (Berl). 1997 Feb;129(4):365-71

[4]Allen AR, Singh A, Zhuang ZP, Kung MP, Kung HF, Lucki I. The 5-HT1A receptor antagonist p-MPPI blocks responses mediated by postsynaptic and presynaptic 5-HT1A receptors. Pharmacol Biochem Behav. 1997 May-Jun;57(1-2):301-7

[5]Popova NK, Ivanova EA. 5-HT(1A) receptor antagonist p-MPPI attenuates acute ethanol effects in mice and rats. Neurosci Lett. 2002 Mar 29;322(1):1-4