Betahistine 2HCl

Catalog No.S3176 Synonyms: PT-9

Betahistine 2HCl Chemical Structure

Molecular Weight(MW): 209.12

Betahistine is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Betahistine 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

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)

* 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.

Chemical Information

Molecular Weight 209.12
Formula

C8H12N2.2HCl

CAS No. 5579-84-0
Storage powder
Synonyms PT-9

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02026778 Unknown status Nausea and Vomiting Yonsei University December 2013 --
NCT01468285 Completed Gait or Balance Disorder Problems Abbott Products|Abbott February 2012 Phase 4
NCT01168336 Completed Healthy OBEcure Ltd. July 2010 Phase 1
NCT00852956 Completed Healthy OBEcure Ltd. February 2009 Phase 1
NCT00829881 Completed Attention Deficit Disorder With Hyperactivity P2D, Inc.|National Institute of Mental Health (NIMH) January 2009 Phase 1
NCT00748436 Completed Obesity OBEcure Ltd.|International Antiviral Therapy Evaluation Center September 2008 Phase 2

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.

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID