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

Betahistine 

Cat. No.: HY-B0524 Purity: >98.0%
Handling Instructions

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

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

Betahistine Chemical Structure

Betahistine Chemical Structure

CAS No. : 5638-76-6

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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

H1 Receptor

 

H3 receptor

 

In Vitro

Betahistine (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 (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 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 inhibits cAMP formation with an EC50 value of 0.1 μM in CHO (rH3(445)R) and full agonist activity[2].

In Vivo

Betahistine (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 (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

136.19

Formula

C₈H₁₂N₂

CAS No.

5638-76-6

SMILES

CNCCC1=NC=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Store at room temperature, keep dry and cool

*In solvent : -80°C, 6 months; -20°C, 1 month (Store at room temperature, keep dry and cool)

References
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Keywords:

BetahistineHistamine ReceptorantipsychoticepisodeschizophreniaRheumatoidarthritisRACIAMénièrediseaseInhibitorinhibitorinhibit

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Betahistine
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