Niaprazine

Research use only, not for human use.

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.

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.

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.

Nopron | 1709 CERM

Endocrinology/Hormones

5-HT Receptor

——

——

——

27367-90-4

356.445

C20H25FN4O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (280.55 mM)

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

——

(-20℃)

With Ice Pack

≥ 2 years