Niaprazine

Name: Niaprazine
Brand: MedChemExpress
SKU: HY-105542
Rating: 4.5 (1 reviews)

Cat. No.: HY-105542 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research.

For research use only. We do not sell to patients.

Niaprazine Chemical Structure

CAS No. : 27367-90-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Niaprazine:

Niaprazine (Standard) Get quote

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Biological Activity
Purity & Documentation
References
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Description

Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research^[1]^[2].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

356.44

Formula

C₂₀H₂₅FN₄O

CAS No.

27367-90-4

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (280.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8055 mL	14.0276 mL	28.0552 mL
5 mM	0.5611 mL	2.8055 mL	5.6110 mL
10 mM	0.2806 mL	1.4028 mL	2.8055 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (2.33 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.83 mg/mL (2.33 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 0.83 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.83 mg/mL (2.33 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (271 KB) SDS (251 KB)

COA (244 KB) HNMR (274 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[1]. D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001. [Content Brief]

[2]. P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8055 mL	14.0276 mL	28.0552 mL	70.1380 mL
	5 mM	0.5611 mL	2.8055 mL	5.6110 mL	14.0276 mL
	10 mM	0.2806 mL	1.4028 mL	2.8055 mL	7.0138 mL
	15 mM	0.1870 mL	0.9352 mL	1.8703 mL	4.6759 mL
	20 mM	0.1403 mL	0.7014 mL	1.4028 mL	3.5069 mL
	25 mM	0.1122 mL	0.5611 mL	1.1222 mL	2.8055 mL
	30 mM	0.0935 mL	0.4676 mL	0.9352 mL	2.3379 mL
	40 mM	0.0701 mL	0.3507 mL	0.7014 mL	1.7535 mL
	50 mM	0.0561 mL	0.2806 mL	0.5611 mL	1.4028 mL
	60 mM	0.0468 mL	0.2338 mL	0.4676 mL	1.1690 mL
	80 mM	0.0351 mL	0.1753 mL	0.3507 mL	0.8767 mL
	100 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7014 mL

Niaprazine Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Niaprazine27367-90-4Histamine ReceptorH1-receptorsleepdisorderssedativeautistic5-HIAA5-HT2Inhibitorinhibitorinhibit

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Niaprazine

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Other Forms of Niaprazine:

Niaprazine Related Antibodies

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•Related Small Molecules:

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View All Histamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Niaprazine Related Antibodies

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Complete Stock Solution Preparation Table

Niaprazine Related Classifications

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