For research use only.
Catalog No.S3176 Synonyms: PT-9
Molecular Weight(MW): 209.12
Betahistine is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
|Description||Betahistine is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.|
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. |
|In vitro||DMSO||38 mg/mL (181.71 mM)|
|Water||38 mg/mL (181.71 mM)|
|Ethanol||1 mg/mL (4.78 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (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.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00852956||Completed||Drug: Betahistine||Healthy||OBEcure Ltd.||February 2009||Phase 1|
|NCT00585585||Terminated||Drug: betahistine dihydrochloride||Recurrent Major Depressive Disorder With Atypical Features||University of Cincinnati||July 2007||Phase 2|
|NCT00459992||Completed||Drug: Betahistine Hydrochloride||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|
|NCT00428168||Terminated||Drug: Betahistine||Weight Gain||OBEcure Ltd.||March 2007||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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