Betahistine 2HCl

Alias: PT-9; Betahistine dihydrochloride; Betahistine HCl; PT 9; PT9; trade names Veserc, Serc; Hiserk; Betaserc; Vergo

Cat No.:V1236 Purity: ≥98%

COA Product Data Instructions for use SDS

Betahistine 2HCl Chemical Structure CAS No.: 5579-84-0
Product category: Histamine Receptor

This product is for research use only, not for human use. We do not sell to patients.

Size	Price	Stock	Qty
500mg
1g
5g
10g
Other Sizes

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Betahistine dihydrochloride (formerly PT 9; PT9; trade names Veserc, Serc, Hiserk, Betaserc, Vergo), the dihydrochloride salt of Betahistine which was pproved in EU in 1970s for treating Ménière's disease, is a potent antagonist of histamine H3 receptor used as an anti-vertigo drug. It inhibits the histamine H3 receptor with an IC50 of 1.9 μM. Betahistine has been prescribed frequently to treat balance issues or to lessen the symptoms of vertigo linked to Ménière's disease.

Biological Activity I Assay Protocols (From Reference)

Targets

Histamine H3 receptor ( IC50 = 1.9 μM )

ln Vitro

In vitro activity: Betahistine dihydrochloride (0-10 μM) inhibits [¹²⁵I]iodoproxyfan binding to membranes of CHO (rH₃₍₄₄₅₎R) and CHO (hH₃₍₄₄₅₎R) cells with IC50 values of 1.9 μM and 3.3 μM, respectively. In CHO (rH₃₍₄₄₅₎R), CHO (rH₃₍₄₄₅₎R, and CHO (hH₃₍₄₄₅₎R) cells, betahistine dihydrochloride (0–10 μM) regulates the formation of cAMP. Betahistine gradually increases cAMP formation at low concentrations, with EC50 values of 0.1 nM, 0.05 nM, and 0.3 nM, respectively. It exhibits apparent inverse agonist behavior. Conversely, betahistine suppresses cAMP formation and full agonist activity at concentrations greater than 10 nM, with an EC50 value of 0.1 μM in CHO (rH₃₍₄₄₅₎R)[2].

ln Vivo

Betahistine dihydrochloride (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) an ED50 of 0.4 mg/kg, acute administration has raised tele-methylhistamine (t-MeHA) levels, suggesting the opposite agonism. Additionally, in male Swissmice, it raises t-MeHA levels with an ED50 of 2 mg/kg following acute oral administration[2].
Betahistine dihydrochloride (oral administration; 1 and 5 mg/kg; daily for 3 weeks) decreases the amount of pro-inflammatory cytokines and lessens the severity of arthritis in the paw tissues of CIA mice[3].

Animal Protocol

Collagen-induced arthritis (CIA) DBA/1 male mouse model
1 mg/kg; 5mg/kg
Oral adminstration; day 21 to day 42 after a 21-day CIA induction

References

[1]. The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3.

[2]. Effects of betahistine at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54.

[3]. Betahistine attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C8H12N2.2HCL
Molecular Weight	209.12
Exact Mass	208.05
Elemental Analysis	C, 45.95; H, 6.75; Cl, 33.90; N, 13.40
CAS #	5579-84-0
Related CAS #	Betahistine; 5638-76-6; Betahistine-d3 dihydrochloride; 244094-72-2; Betahistine mesylate; 54856-23-4; Betahistine-13C,d3 dihydrochloride
Appearance	Solid powder
SMILES	CNCCC1=CC=CC=N1.Cl.Cl
InChi Key	XVDFMHARQUBJRE-UHFFFAOYSA-N
InChi Code	InChI=1S/C8H12N2.2ClH/c1-9-7-5-8-4-2-3-6-10-8;;/h2-4,6,9H,5,7H2,1H3;2*1H
Chemical Name	N-methyl-2-pyridin-2-ylethanamine;dihydrochloride
Synonyms	PT-9; Betahistine dihydrochloride; Betahistine HCl; PT 9; PT9; trade names Veserc, Serc; Hiserk; Betaserc; Vergo
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1) .This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 33.3~38 mg/mL (159.4~181.7 mM)

Water: ~38 mg/mL (~181.7 mM)

Ethanol: <1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: 150 mg/mL (717.29 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.7819 mL	23.9097 mL	47.8194 mL
	5 mM	0.9564 mL	4.7819 mL	9.5639 mL
	10 mM	0.4782 mL	2.3910 mL	4.7819 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00160238	Completed	Drug: Betahistine 24 mg bid (Betaserc)	Meniere's Disease	Solvay Pharmaceuticals	January 2003	Phase 4
NCT00459992	Completed	Drug: Betahistine Hydrochloride	Obesity Overweight	Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	April 10, 2007	Phase 1
NCT05938517	Completed	Drug: Betahistine dihydrochloride Drug: Selegiline-hydrochloride	Ménière's Disease	Ludwig-Maximilians - University of Munich	June 2, 2021	Phase 1
NCT01468285	Completed	Drug: betahistine dihydrochloride Other: placebo	Gait or Balance Disorder Problems	Abbott Products	February 2012	Phase 4
NCT00829881	Completed	Drug: Betahistine Hydrochloride Drug: Placebo Capsule	Attention Deficit Disorder With Hyperactivity	P2D, Inc.	January 2009	Phase 1