Niaprazine

Modify Date: 2025-08-25 06:54:05

Niaprazine Structure
Niaprazine structure
Common Name Niaprazine
CAS Number 27367-90-4 Molecular Weight 356.43700
Density N/A Boiling Point N/A
Molecular Formula C20H25FN4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Niaprazine


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].

 Names

Name N-[4-[4-(4-fluorophenyl)piperazin-1-yl]butan-2-yl]pyridine-3-carboxamide
Synonym More Synonyms

 Niaprazine Biological Activity

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].
Related Catalog
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].
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.
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.

 Chemical & Physical Properties

Molecular Formula C20H25FN4O
Molecular Weight 356.43700
Exact Mass 356.20100
PSA 51.96000
LogP 3.12900

 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 DATA

ACUTE 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

 Safety Information

Hazard Codes Xi
HS Code 2933599090

 Customs

HS Code 2933599090
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%

 Synonyms

Nopron
EINECS 248-431-5
1709 CERM
Niaprazine
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