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)|
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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|
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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