Betahistine 2HCl

For research use only.

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.

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10mM (1mL 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.
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]


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


CAS No. 5579-84-0
Storage powder
in solvent
Synonyms PT-9
Smiles Cl.Cl.CNCCC1=NC=CC=C1

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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

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID