Betahistine dihydrochloride
Based on 2 publication(s) in Google Scholar
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.
- Purity: 99.82%
- CAS No.: 5579-84-0
- Formula: C8H14Cl2N2
- Molecular Weight:209.12
-
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Immunology/Inflammation Compound Library
HY-L007
-
Neuronal Signaling Compound Library
HY-L013
-
FDA-Approved Drug Library
HY-L022
-
Drug Repurposing Compound Library
HY-L035
-
Endocrinology Compound Library
HY-L047
-
Anti-COVID-19 Compound Library
HY-L052
-
NMPA-Approved Drug Library
HY-L053
-
Orally Active Compound Library
HY-L061
-
Neurotransmitter Receptor Compound Library
HY-L062
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Targeted Diversity Library
HY-L099
-
Human Metabolite Library
HY-L123
-
Coagulation and Anti-coagulation Compound Library
HY-L136
-
Heterocyclic Compound Library
HY-L138
-
Off-patent Drug Library
HY-L141
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) Betahistine dihydrochloride
MoreAll Histamine Receptor Isoforms
More
Biological Activity
|
H3 Receptor |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (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.
Chemical Information
-
CAS No. 5579-84-0
-
Appearance Solid
-
Molecular Weight 209.12
-
Formula C8H14Cl2N2
-
Color White to off-white
-
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)
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Pharm Res
Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]2025 Aug;42(8):1315-1329. PMID: 40760405 -
Brain Sci
Combination Lorcaserin and Betahistine Treatment Improves Cognitive Dysfunction and Dopaminergic Neuron Activity in a Rat Model of Diet-Induced Obesity. [Abstract]2025 Aug 25;15(9):913. PMID: 41008273
Solvent & Solubility
H2O : ≥ 50 mg/mL (239.10 mM)
DMSO : 33.33 mg/mL (159.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 5 mg/mL (23.91 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 150 mg/mL (717.29 mM); Clear solution; Need ultrasonic
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
Handling Instructions (2659 KB)
References
[1]. Poyurovsky M, et al. The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3. [Content Brief]
[2]. Gbahou F, et al. Effects of betahistine at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54. [Content Brief]
[3]. Tang KT, et al. Betahistine attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF / DMSO / H2O | 1 mM | 4.7819 mL | 23.9097 mL | 47.8194 mL | 119.5486 mL |
| 5 mM | 0.9564 mL | 4.7819 mL | 9.5639 mL | 23.9097 mL | |
| 10 mM | 0.4782 mL | 2.3910 mL | 4.7819 mL | 11.9549 mL | |
| 15 mM | 0.3188 mL | 1.5940 mL | 3.1880 mL | 7.9699 mL | |
| 20 mM | 0.2391 mL | 1.1955 mL | 2.3910 mL | 5.9774 mL | |
| DMSO / H2O | 25 mM | 0.1913 mL | 0.9564 mL | 1.9128 mL | 4.7819 mL |
| 30 mM | 0.1594 mL | 0.7970 mL | 1.5940 mL | 3.9850 mL | |
| 40 mM | 0.1195 mL | 0.5977 mL | 1.1955 mL | 2.9887 mL | |
| 50 mM | 0.0956 mL | 0.4782 mL | 0.9564 mL | 2.3910 mL | |
| 60 mM | 0.0797 mL | 0.3985 mL | 0.7970 mL | 1.9925 mL | |
| 80 mM | 0.0598 mL | 0.2989 mL | 0.5977 mL | 1.4944 mL | |
| 100 mM | 0.0478 mL | 0.2391 mL | 0.4782 mL | 1.1955 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Betahistine dihydrochloride Related Classifications
HY-B0524A Related Classifications
Powered by Bioz