Niaprazine

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Niaprazine is a histamine H1-receptor antagonist with marked sedative properties.

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties.(In Vitro):Niaprazine, particularly the (+)stereoisomer, has a higher affinity for alpha 1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites (Ki sigma mciroM).(In Vivo):Niaprazine (60 mg/kg i.p.) increased rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Rat brain 5-hydroxytryptamine (5-HT) levels were unchanged. Niaprazine also produced a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA). Pretreatment with alpha-phenyl-alpha-propyl-benzeneacetic acid, 2-(diethylamino) ethyl ester hydrochloride (SKF 525A) (75 mg/kg i.p.) potentiated the increase in 5-HIAA and depletion of catecholamines produced 1 hr after niaprazine, but abolished the reduction in 5-HIAA produced 8 hr after the drug.

Nopron; 1709 CERM

Endocrinology/Hormones

5-HT Receptor

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27367-90-4

356.4

C20H25FN4O

>98% (HPLC)

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CC(CCN1CCN(CC1)c1ccc(F)cc1)NC(=O)c1cccnc1

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(-20℃)

With Ice Pack

≥ 2 years