Bioactivity:

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]. Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, _2, _, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for _1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites[2]. 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]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3] [1]. D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001. [2]. P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50. [3]. P E Keane, et al. The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain. Neuropharmacology. 1982 Feb;21(2):163-9.

CAS nr:

27367-90-4

Purity:

98%

Molecular Weight:

356,44

SMILES:

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

Formula:

C20H25FN4O

Pathway:

Immunology/Inflammation,Neuroscience,GPCR/G Protein,Neuroscience,Neuroscience,GPCR/G Protein,GPCR/G Protein

Target:

Histamine Receptor,Histamine Receptor,5-HT Receptor,5-HT Receptor,Adrenergic Receptor,Adrenergic Receptor,Histamine Receptor