Introduction：Basic information about CAS 27367-90-4|Niaprazine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Niaprazine |
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| CAS Number | 27367-90-4 | Molecular Weight | 356.43700 |
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| Density | / | Boiling Point | / |
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| Molecular Formula | C20H25FN4O | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | N-[4-[4-(4-fluorophenyl)piperazin-1-yl]butan-2-yl]pyridine-3-carboxamide |
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| Synonym | More Synonyms |
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Niaprazine BiologicalActivity
| Description | 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]. |
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| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
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| In Vitro | 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[2]. |
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| In Vivo | 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] 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. |
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| References | [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. |
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Chemical & Physical Properties
| Molecular Formula | C20H25FN4O |
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| Molecular Weight | 356.43700 |
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| Exact Mass | 356.20100 |
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| PSA | 51.96000 |
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| LogP | 3.12900 |
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| InChIKey | RSKQGBFMNPDPLR-UHFFFAOYSA-N |
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| SMILES | CC(CCN1CCN(c2ccc(F)cc2)CC1)NC(=O)c1cccnc1 |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- QS4476100
- CHEMICAL NAME :
- Nicotinamide, N-(3-(4-(p-fluorophenyl)-1-piperazinyl)-1-methylpropy l)-
- CAS REGISTRY NUMBER :
- 27367-90-4
- BEILSTEIN REFERENCE NO. :
- 0844157
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 2
- MOLECULAR FORMULA :
- C20-H25-F-N4-O
- MOLECULAR WEIGHT :
- 356.49
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 890 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #1957371
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 145 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #1957371
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Safety Information
| Hazard Codes | Xi |
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| HS Code | 2933599090 |
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Customs
| HS Code | 2933599090 |
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| Summary | 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| Nopron |
| EINECS 248-431-5 |
| 1709 CERM |
| Niaprazine |
