product name Betahistine 2HCl
Description: Betahistine dihydrochloride (also known as PT-9), the HCL salt of Betahistine, is a histamine H3 receptor inhibitor with IC50 of 1.9 μM. Betahistine dihydrochloride is an anti-vertigo drug. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms associated with Ménières disease. It was first approved in Europe in 1970 for the treatment of Ménières disease.
References: J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54; Eur Arch Otorhinolaryngol. 2003 Feb;260(2):73-7.
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)
Synonyms
PT-9
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427762
| 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. Kinase Assay: Cell Assay: |
|---|---|
| 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 Menieres 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 Menieres 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 | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54; Eur Arch Otorhinolaryngol. 2003 Feb;260(2):73-7. |
