Betahistine 2HCl - Moligand™, 10mM in DMSO , CAS No.5579-84-0
Disponible
SKU
B408529
H3 receptor Selective Inhibitors | Antagonists
Information
Betahistine (PT-9) is ahistamine H3receptor inhibitor withIC50of 1.9 μM.
In vitro
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 Meni鑢e\'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.
Cell Data
cell lines：Calu-6 cells
Concentrations：
Incubation Time：
Powder Purity:≥99%
Más Información
| CAS | 5579-84-0 |
|---|---|
| Concentración | 10mM in DMSO |
| Sinónimos | PT-9 | N-methyl-2-(pyridin-2-yl)ethanamine dihydrochloride |
| Especificaciones y pureza | Moligand™, 10mM in DMSO |
| Condiciones de almacenamiento de almacenamiento | Store at -80°C |
| Enviado en | Dry ice packs + Cold packs |
| Product Description | Information Betahistine (PT-9) is ahistamine H3receptor inhibitor withIC50of 1.9 μM. 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 Meni鑢e\'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. cell lines：Calu-6 cells Concentrations： Incubation Time： Powder Purity:≥99% |
| Solubilidad | Solubility (25°C) In vitro Water: 36 mg/mL (199.82 mM); DMSO: Insoluble; |
| Número CE | 226-966-5 |
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