27367-90-4
27367-90-4 結(jié)構(gòu)式
基本信息
中文別名
尼普拉嗪 英文別名
Nopron1709 CERM
Niaprazine
N-(4-(4-(4-FLUOROPHENYL)PIPERAZIN-1-YL)BUTAN-2-YL)NICOTINAMIDE
N-[3-[4-(p-Fluorophenyl)-1-piperazinyl]-1-methylpropyl]nicotinamide
N-[3-[4-(4-Fluorophenyl)-1-piperazinyl]-1-methylpropyl]nicotinamide
N-[3-[4-(4-Fluorophenyl)-1-piperazinyl]-1-methylpropyl]-3-pyridinecarboxamide
3-Pyridinecarboxamide, N-[3-[4-(4-fluorophenyl)-1-piperazinyl]-1-methylpropyl]-
物理化學(xué)性質(zhì)
熔點(diǎn)131℃
密度1.165
儲存條件-20°C儲存
溶解度DMSO: 100 mg/mL (280.55 mM)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
Niaprazine 是一種具有強(qiáng)效鎮(zhèn)靜作用的組胺 H1 受體 (histamine H1-receptor) 拮抗劑。Niaprazine 具有抗組胺和抗血清素活性，并可用于睡眠障礙的研究。體外研究
Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, α2, β, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites.
體內(nèi)研究
Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Niaprazine also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA).
| Animal Model: | Male Sprague-Dawley rats (150-200 g) |
| Dosage: | 60 mg/kg |
| Administration: | Intraperitoneal injection; once |
| Result: | Increased rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. |