1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Niaprazine

Niaprazine 

Cat. No.: HY-105542
Handling Instructions

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research.

For research use only. We do not sell to patients.

Niaprazine Chemical Structure

Niaprazine Chemical Structure

CAS No. : 27367-90-4

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Description

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2].

In Vitro

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (150-200 g)[3]
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.
Molecular Weight

356.44

Formula

C₂₀H₂₅FN₄O

CAS No.

27367-90-4

SMILES

O=C(C1=CN=CC=C1)NC(C)CCN2CCN(C3=CC=C(F)C=C3)CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

NiaprazineHistamine ReceptorH1-receptorsleepdisorderssedativeautistic5-HIAA5-HT2Inhibitorinhibitorinhibit

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Niaprazine
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