CAS Number5638-76-6
Synonyms2-(b-Methylaminoethyl)pyridine; N-methyl-2-pyridin-2-ylethanamine; MFCD00006362; N-Methyl-2-(2-pyridinyl)ethanamine; EINECS 227-086-4; Suzutolon; 2-(2-Methylaminoethyl)pyridine; N-methyl-2-(pyridin-2-yl)ethanamine; N-Methyl-2-pyridineethanamine; Betahistine
Molecular FormulaC8H12N2
Molecular Weight136.19
Purity97%
Density1.0±0.1 g/cm3
Boiling Point113-114 °C/30 mmHg (lit.)
Appearancelight yellow
EINECS227-086-4
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 5638-76-6 |
| Catalog No. | 2A-9059551 |
| Chinese Name | 倍他司汀 |
| Synonyms | 2-(b-Methylaminoethyl)pyridine; N-methyl-2-pyridin-2-ylethanamine; MFCD00006362; N-Methyl-2-(2-pyridinyl)ethanamine; EINECS 227-086-4; Suzutolon; 2-(2-Methylaminoethyl)pyridine; N-methyl-2-(pyridin-2-yl)ethanamine; N-Methyl-2-pyridineethanamine; Betahistine |
| Molecular Formula | C8H12N2 |
| Molecular Weight | 136.19 |
| Purity | 97 |
| Density | 1.0±0.1 g/cm3 |
| Boiling Point | 113-114 °C/30 mmHg (lit.) |
| Appearance | light yellow |
| Storage Condition | Store in a cool and dry place |
| Application | Betahistine is an orally active histamine H1 receptor agonist and H3 receptor antagonist. Betahistine may be used in research on rheumatoid arthritis (RA). |
| EINECS | 227-086-4 |
| HTC | 2933399090 |
| PubChem ID | 24896774 |
| MDL Number | MFCD00006362 |
| SMILES | CNCCc1ccccn1 |
| InChI | 1S/C8H12N2/c1-9-7-5-8-4-2-3-6-10-8/h2-4,6,9H,5,7H2,1H3 |
| InChI Key | UUQMNUMQCIQDMZ-UHFFFAOYSA-N |
| NACRES Code | NA.22 |
| UNSPSC | 12352100 |
| Hazard Symbols | transportation |
| Bioactivity | 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]. Related Catalog Research Areas >> Cancer Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Target 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. 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. [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. [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. Chemical & Physical Properties Density 1.0±0.1 g/cm3 Boiling Point 210.9±15.0 °C at 760 mmHg Molecular Formula C8H12N2 Molecular Weight 136.194 Flash Point 96.7±0.0 °C Exact Mass 136.100052 PSA 24.92000 LogP 0.10 Vapour Pressure 0.2±0.4 mmHg at 25°C Index of Refraction 1.510 InChIKey UUQMNUMQCIQDMZ-UHFFFAOYSA-N SMILES CNCCc1ccccn1 Storage condition -20℃ |
| Use of | 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]. Properties Articles27 Name betahistine Synonym More Synonyms Betahistine Biological Activity 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]. Related Catalog Research Areas >> Cancer Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor 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]. 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. [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. Chemical & Physical Properties Molecular Formula C8H12N2 Exact Mass 136.100052 PSA 24.92000 Index of Refraction 1.510 InChIKey UUQMNUMQCIQDMZ-UHFFFAOYSA-N Storage condition -20℃ |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Shipping Name: UN |
| MSDS Transport Info | Module 14. Shipping information 14.1 UN dangerous goods number European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.2 United Nations shipping name European Land Transport Dangerous Regulations: Non-dangerous goods IMDG Code: Non-dangerous goods International air transport dangerous goods regulations: non-dangerous goods 14.3 Transport hazard categories European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.4 Package group European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.5 Environmental hazards European Land Transport Danger Regulations: No International Maritime Danger Regulations International Air Transport Danger Regulations: No Marine pollutants (yes/no): No 14.6 Special reminder to users No data available |
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