1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Betahistine mesylate

Betahistine mesylate 

Cat. No.: HY-D0237 Purity: >98.0%
Handling Instructions

Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine mesylate is used for the study of rheumatoid arthritis (RA).

For research use only. We do not sell to patients.

Betahistine mesylate Chemical Structure

Betahistine mesylate Chemical Structure

CAS No. : 54856-23-4

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Based on 1 publication(s) in Google Scholar

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Description

Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine mesylate is used for the study of rheumatoid arthritis (RA)[3].

In Vitro

Betahistine mesylate (0-10 μM) inhibits [125I]iodoproxyfan binding to membranes of CHO (rH3(445)R) and CHO (hH3(445)R) cells with IC50 values of 1.9 μM and 3.3 μM, respectively. Lead to Ki values of 1.4 μM and 2.5 μM, respectively[2].
Betahistine mesylate (0-10 μM) has a regulating function on cAMP formation in CHO (rH3(445)R), CHO (rH3(413)R), and CHO (hH3(445)R) cells. At low concentrations, Betahistine mesylate behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC50 values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, Betahistine mesylate inhibits cAMP formation with an EC50 value of 0.1 μM in CHO (rH3(445)R) and full agonist activity[2].

In Vivo

Betahistine mesylate (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED50 of 2 mg/kg in male Swissmice[2].
Betahistine mesylate (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice[3].

Animal Model: Collagen-induced arthritis (CIA) DBA/1 male mouse model[3]
Dosage: 1 mg/kg; 5mg/kg
Administration: Oral adminstration; day 21 to day 42 after a 21-day CIA induction
Result: Ameliorated mouse CIA by decreasing joint destruction.
Molecular Weight

328.41

Formula

C₁₀H₂₀N₂O₆S₂

CAS No.

54856-23-4

SMILES

CNCCC1=NC=CC=C1.CS(=O)(O)=O.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

References
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Keywords:

BetahistineHistamine ReceptorInhibitorinhibitorinhibit

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Betahistine mesylate
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