| CAS NO: | 5579-84-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| 25g | 电议 |
| Molecular Weight (MW) | 209.12 |
|---|---|
| Formula | C8H12N2.2HCl |
| CAS No. | 5579-84-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 38 mg/mL (181.7 mM) |
| Water: 38 mg/mL (181.7 mM) | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | Chemical Name: Methyl[2-(2-pyridyl)ethyl]amine dihydrochloride SMILES Code: CNCCC1=NC=CC=C1.[H]Cl.[H]Cl |
| Synonyms | PT-9; Betahistine dihydrochloride; Betahistine HCl; PT 9; PT9; trade names Veserc, Serc, Hiserk, Betaserc, Vergo. |
| In Vitro | In vitro activity: Betahistine progressively enhances cAMP formation with a maximal effect, observed up to 10 nM, in CHO(H3R) cells incubated with 3 μM forskolin. In contrast, at concentrations higher than 10 nM betahistine progressively inhibits cAMP formation in CHO(H3R) cells incubated with 3 μM forskolin. Betahistine progressively reduces A23187-evoked [3H]arachidonic acid release (EC50=0.1 nM) with a maximal effect, observed up to 30 nM A23187-evoked [3H]arachidonic acid release from CHO(H3R) cells. Betahistine progressively enhanced the release of A23187-evoked [3H]arachidonic acid from CHO(H3R) cells at concentrations higher than 30 NM. |
|---|---|
| In Vivo | Betahistine (< 30 mg/kg) increases t-MeHA levels in a dose-dependent manner with an ED50 of 2 mg/kg and a maximal effect of ~35% reached at 30 mg/kg in mouse brain. Betahistine (16 mg twice per day for 3 months) has a significant effect on the frequency, intensity and duration of vertigo attacks, associated symptoms and the quality of life also are significantly improved in patients with Meniere's disease. Betahistine-dihydrochloride (16 mg tid and 48 mg tid) shows that the number of attacks per month decreased in both doses over time in Meniere's disease. Betahistine (50 mg/kg) treatment induces symmetrical changes with up-regulation of histidine decarboxylase mRNA in the tuberomammillary nucleus and reduction of [3H]N-alpha-methylhistamine labeling in both the tuberomammillary nucleus, the vestibular nuclei complex and nuclei of the inferior olive in brain sections of cats. |
| Animal model | Mice |
| Formulation & Dosage | 30 mg/kg |
| References | J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54; Eur Arch Otorhinolaryngol. 2003 Feb;260(2):73-7. |
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