Eltoprazine (Synonyms: DU 28853)

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Data Sheet SDS COA Handling Instructions

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Eltoprazine (DU 28853) is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine shows antiaggressive and anxiogenic effects.

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Eltoprazine Chemical Structure

CAS No. : 98224-03-4

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Other In-stock Forms of Eltoprazine:

Eltoprazine hydrochloride

Other Forms of Eltoprazine:

Eltoprazine hydrochloride In-stock
Eltoprazine dihydrochloride Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Eltoprazine (DU 28853) is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine shows antiaggressive and anxiogenic effects^[1]^[2].

IC₅₀ & Target

5-HT_1A Receptor

5-HT_1B Receptor

5-HT_2C Receptor

In Vivo

Rats are chronically treated with Mianserin (10 mg/kg i.p.) or Eltoprazine (1 mg/kg i.p.) and are tested in the elevated plus-maze test for anxiety. Mianserin and Eltoprazine display opposite effects in the elevated plus-maze: Mianserin induces anxiolytic-like effects, while Eltoprazine shows anxiogenic-like ones^[2].

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

Clinical Trial

Molecular Weight

220.27

Formula

C₁₂H₁₆N₂O₂

CAS No.

98224-03-4

Appearance

Solid

Color

White to off-white

SMILES

N1(C2=C3OCCOC3=CC=C2)CCNCC1

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 : ≥ 25 mg/mL (113.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.5399 mL	22.6994 mL	45.3988 mL
5 mM	0.9080 mL	4.5399 mL	9.0798 mL
10 mM	0.4540 mL	2.2699 mL	4.5399 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: ≥ 2.5 mg/mL (11.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: ≥95.0%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (249 KB)

Handling Instructions (2659 KB)

References

[1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [Content Brief]

[2]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	4.5399 mL	22.6994 mL	45.3988 mL	113.4971 mL
	5 mM	0.9080 mL	4.5399 mL	9.0798 mL	22.6994 mL
	10 mM	0.4540 mL	2.2699 mL	4.5399 mL	11.3497 mL
	15 mM	0.3027 mL	1.5133 mL	3.0266 mL	7.5665 mL
	20 mM	0.2270 mL	1.1350 mL	2.2699 mL	5.6749 mL
	25 mM	0.1816 mL	0.9080 mL	1.8160 mL	4.5399 mL
	30 mM	0.1513 mL	0.7566 mL	1.5133 mL	3.7832 mL
	40 mM	0.1135 mL	0.5675 mL	1.1350 mL	2.8374 mL
	50 mM	0.0908 mL	0.4540 mL	0.9080 mL	2.2699 mL
	60 mM	0.0757 mL	0.3783 mL	0.7566 mL	1.8916 mL
	80 mM	0.0567 mL	0.2837 mL	0.5675 mL	1.4187 mL
	100 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1350 mL

Eltoprazine 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:

Eltoprazine98224-03-4DU 28853DU28853DU-288535-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1A5-HT1B5-HT2Cantiaggressive and anxiogenic effectsInhibitorinhibitorinhibit

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