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

Betahistine dihydrochloride 

Cat. No.: HY-B0524A Purity: 99.74%
Handling Instructions

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

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

Betahistine dihydrochloride Chemical Structure

Betahistine dihydrochloride Chemical Structure

CAS No. : 5579-84-0

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
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Description

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

IC50 & Target[1]

H3 Receptor

 

In Vitro

Betahistine dihydrochloride (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 dihydrochloride (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Betahistine dihydrochloride (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 dihydrochloride (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

209.12

Formula

C₈H₁₄Cl₂N₂

CAS No.

5579-84-0

SMILES

CNCCC1=CC=CC=N1.Cl.Cl

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)

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (239.10 mM)

DMSO : 33.33 mg/mL (159.38 mM; Need ultrasonic)

DMF : 5 mg/mL (23.91 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7819 mL 23.9097 mL 47.8194 mL
5 mM 0.9564 mL 4.7819 mL 9.5639 mL
10 mM 0.4782 mL 2.3910 mL 4.7819 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 150 mg/mL (717.29 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

BetahistineHistamine ReceptorantipsychoticepisodeschizophreniaRheumatoidarthritisRACIAMénièrediseaseInhibitorinhibitorinhibit

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Betahistine dihydrochloride
Cat. No.:
HY-B0524A
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