CAS Number54856-23-4
Synonyms2-Pyridineethanamine, N-methyl-, methanesulfonate (1:2); N-Methyl-2-pyridineethanamine Dimethanesulfonate; MFCD00211321; N-Methyl-2-(2-pyridinyl)ethanamine methanesulfonate (1:2); EINECS 259-377-7; N-Methyl-2-(pyridin-2-yl)ethanamine methanesulfonate (1:2); methanesulfonic acid,N-methyl-2-pyridin-2-ylethanamine
Molecular FormulaC10H20N2O6S2
Molecular Weight328.41
Purity99%
Boiling Point210.9ºC at 760 mmHg
Melting Point112°C
AppearanceSolid;White to Almost white powder to crystal
EINECS259-377-7
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 54856-23-4 |
| Catalog No. | 2A-9008776 |
| Chinese Name | 甲磺酸倍他司汀 |
| Synonyms | 2-Pyridineethanamine, N-methyl-, methanesulfonate (1:2); N-Methyl-2-pyridineethanamine Dimethanesulfonate; MFCD00211321; N-Methyl-2-(2-pyridinyl)ethanamine methanesulfonate (1:2); EINECS 259-377-7; N-Methyl-2-(pyridin-2-yl)ethanamine methanesulfonate (1:2); methanesulfonic acid,N-methyl-2-pyridin-2-ylethanamine |
| Molecular Formula | C10H20N2O6S2 |
| Molecular Weight | 328.41 |
| Purity | 99 |
| Boiling Point | 210.9ºC at 760 mmHg |
| Melting Point | 112°C |
| Appearance | Solid;White to Almost white powder to crystal |
| Storage Condition | Keep the receptacle sealed, stored in a cool, dry |
| Application | Betahistine mesylate is an orally active histamine H1 receptor agonist and H3 receptor antagonist. Betahistine may be used in research on rheumatoid arthritis (RA). |
| EINECS | 259-377-7 |
| HTC | 2933399090 |
| MDL Number | MFCD00211321 |
| SMILES | [S](=O)(=O)(O)C.[S](=O)(=O)(O)C.N(CCc1ncccc1)C |
| InChI | 1S/C8H12N2.2CH4O3S/c1-9-7-5-8-4-2-3-6-10-8;2*1-5(2,3)4/h2-4,6,9H,5,7H2,1H3;2*1H3,(H,2,3,4) |
| InChI Key | ZBJJDYGJCNTNTH-UHFFFAOYSA-N |
| NACRES Code | NA.24 |
| UNSPSC | 41116107 |
| MSDS | msds/8776_1_54856_23_4.pdf |
| Bioactivity | 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]. Related Catalog Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor 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. References [1]. Poyurovsky M, et al. The effect of Betahistine mesylate, 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. [2]. Gbahou F, et al. Effects of Betahistine mesylate 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. [3]. Tang KT, et al. Betahistine mesylate attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245 Chemical & Physical Properties Boiling Point 210.9ºC at 760 mmHg Melting Point 112°C Molecular Formula C10H20N2O6S2 Molecular Weight 328.406 Flash Point 96.7ºC Exact Mass 328.076263 PSA 150.42000 LogP 2.40400 InChIKey ZBJJDYGJCNTNTH-UHFFFAOYSA-N SMILES CNCCc1ccccn1.CS(=O)(=O)O.CS(=O)(=O)O |
| Use of | 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]. Properties Articles25 Name Betahistine Mesylate Synonym More Synonyms Betahistine Mesylate Biological Activity 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]. Related Catalog Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor 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]. References [1]. Poyurovsky M, et al. The effect of Betahistine mesylate, 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. [2]. Gbahou F, et al. Effects of Betahistine mesylate 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. Chemical & Physical Properties Molecular Formula C10H20N2O6S2 Exact Mass 328.076263 PSA 150.42000 LogP 2.40400 InChIKey ZBJJDYGJCNTNTH-UHFFFAOYSA-N |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Purity: 99.0% |
| MSDS Transport Info | Module 14. Shipping information United Nations classification: inconsistent with United Nations classification standards UN number: not specified |
| Related Products in Specialty Chemicals | ||
|---|---|---|
| Sulphoguanidine | 2A-108766 | 2A-9008766 |
| sym-Trimethylbenzene | 108-67-8 | 2A-0202079 |
| Synephrine hydrochloride | 5985-28-4 | 2A-9008770 |
| Tangeretin | 481-53-8 | 2A-9008771 |
| Teflubenzuron | 83121-18-0 | 2A-9008775 |
| tert-Butyl 2-bromoisobutylate | 23877-12-5 | 2A-9008779 |
| tert-Butyl 7-[3-(4-fluorophenyl)-1-isopropyl-2,3-dihydroindol-2-yl]-3,5-dihydroxyhept-6-enoate | 2A-108784 | 2A-9008784 |
| tert-Butyl 7-[3-(4-Fluorophenyl)-1-isopropyl-2,3-dihydroindol-2-yl]-5-hydroxy-3-oxohept-6-enoate | 2A-108785 | 2A-9008785 |
| tert-Butyl N-(4-bromophenyl)carbamate | 131818-17-2 | 2A-9008786 |
| tert-Butyl nitrite | 540-80-7 | 2A-9008787 |
| Browse all Specialty Chemicals products » | ||
Phone:
630-322-8886
630-322-8887
Email:
Office Locations:
Chicago, IL, USA
San Francisco, CA, USA
EN
SDS