Name: Betahistine 2HCl
Brand: Selleck Chemicals
SKU: S3176
Availability: InStock
Rating: 5 (1 reviews)

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Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Ebastine Mianserin HCl Astemizole Ciproxifan Maleate Lafutidine Mizolastine Dimethindene maleate Rupatadine

Solubility

In vitro
Batch:

DMSO : 38 mg/mL (181.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 38 mg/mL

Ethanol : 38 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

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% Tween 80

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	209.12	Formula	C₈H₁₂N₂.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	5579-84-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PT-9			Smiles	CNCCC1=CC=CC=N1.Cl.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Histamine H3 receptor 1.9 μM
In vitro	Betahistine progressively enhances cAMP formation with a maximal effect, observed up to 10 nM, in CHO(H3R) cells incubated with 3 μM forskolin. In contrast, at concentrations higher than 10 nM betahistine progressively inhibits cAMP formation in CHO(H3R) cells incubated with 3 μM forskolin. Betahistine progressively reduces A23187-evoked [³H]arachidonic acid release (EC50=0.1 nM) with a maximal effect, observed up to 30 nM A23187-evoked [³H]arachidonic acid release from CHO(H3R) cells. Betahistine progressively enhanced the release of A23187-evoked [³H]arachidonic acid from CHO(H3R) cells at concentrations higher than 30 nM.
In vivo	Betahistine (< 30 mg/kg) increases t-MeHA levels in a dose-dependent manner with an ED50 of 2 mg/kg and a maximal effect of ∼35% reached at 30 mg/kg in mouse brain. Betahistine (16 mg twice per day for 3 months) has a significant effect on the frequency, intensity and duration of vertigo attacks, associated symptoms and the quality of life also are significantly improved in patients with Meniere's disease. Betahistine-dihydrochloride (16 mg tid and 48 mg tid) shows that the number of attacks per month decreased in both doses over time in Meni鑢e's disease. Betahistine (50 mg/kg) treatment induces symmetrical changes with up-regulation of histidine decarboxylase mRNA in the tuberomammillary nucleus and reduction of [³H]N-alpha-methylhistamine labeling in both the tuberomammillary nucleus, the vestibular nuclei complex and nuclei of the inferior olive in brain sections of cats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20530654/ [2] https://pubmed.ncbi.nlm.nih.gov/12582782/ [3] https://pubmed.ncbi.nlm.nih.gov/18421605/ [4] https://pubmed.ncbi.nlm.nih.gov/12098586/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00852956	Completed	Healthy	OBEcure Ltd.	February 2009	Phase 1
NCT00585585	Terminated	Recurrent Major Depressive Disorder With Atypical Features	University of Cincinnati	July 2007	Phase 2
NCT00459992	Completed	Obesity\|Overweight\|Overnutrition	Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|National Institutes of Health Clinical Center (CC)	April 10 2007	Phase 1

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Betahistine 2HCl Histamine Receptor inhibitor

Chemical Structure

Molecular Weight: 209.12