Niaprazine 是有效的组胺 H1 受体拮抗剂，具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。

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

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)[1].

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[2].

27367-90-4

C20H25FN4O

356.44

DMSO:100 mg/mL (280.55 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years