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编 号:F565997
分子式:C20H25FN4O
分子量:356.44
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research.

体内研究:
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.

体外研究:
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.
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