Betahistine 2HCl

Catalog No.S3176 Synonyms: PT-9

For research use only.

Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.

Betahistine 2HCl Chemical Structure

CAS No. 5579-84-0

Purity & Quality Control

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Biological Activity

Description Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
Targets
Histamine H3 receptor [1]
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. [1]

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. [1] 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. [2] 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. [3] 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. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 38 mg/mL
(181.71 mM)
Water 38 mg/mL
(181.71 mM)
Ethanol 1 mg/mL
(4.78 mM)

Chemical Information

Molecular Weight 209.12
Formula

C8H12N2.2HCl

CAS No. 5579-84-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNCCC1=CC=CC=N1.Cl.Cl

In vivo Formulation Calculator (Clear solution)

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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.
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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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