| Name | Niaprazine |
| Description | Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties. |
| In vitro | Niaprazine demonstrates a low affinity for the vesicular monoamine transporter as well as D2, α2, β, H1, and mAch receptors. Notably, the (+)stereoisomer of Niaprazine shows a significantly higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, whereas it is poorly recognized by 5-HT1A and 5-HT1B binding sites[2]. |
| In vivo | Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 minutes post-treatment but reduces them 3-8 hours after treatment. Niaprazine also temporarily depletes rat brain noradrenaline (NA) and dopamine (DA) levels[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 1 mg/mL (2.81 mM), Sonication is recommended.
DMSO : 100 mg/mL (280.55 mM), Sonication is recommended.
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| Keywords | α1-adrenergic receptor | sleep | sedative | Niaprazine | Inhibitor | inhibit | HistamineReceptor | Histamine Receptor | H1-receptor | H1 receptor | disorders | autistic | AdrenergicReceptor | Adrenergic Receptor | 5HTReceptor | 5-HT2 | 5HT Receptor | 5-HIAA |
| Inhibitors Related | Undecane | Alverine citrate | Meclizine dihydrochloride | Dapoxetine hydrochloride | Cefaclor monohydrate | Famotidine | 1,8-Cineole | Sodium butanoate | Isoprenaline hydrochloride | D-Mannitol | Alginic acid | Cinchonidine |
| Related Compound Libraries | Histamine & Melatonin Receptor-Targeted Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Adrenergic Receptor-Targeted Compound Library | GPCR Compound Library | Anti-Cancer Compound Library |
United States
