Betahistine-d3 is intended for use as an internal standard for the quantification of betahistine by GC- or LC-MS. Betahistine is a histamine H3 receptor antagonist and histamine H1 receptor agonist.1 In vivo, betahistine dilates pre-capillary arterioles and increases blood flow to the stria vascularis in guinea pigs.2,3 Betahistine (8 mg/kg) reduces weight gain and increased feeding behavior induced by olanzapine in female rats.4 Formulations containing betahistine have been used in the treatment of balance disorders and vertigo symptoms associated with Meniere's disease.
1.Timmerman, H.Histamine agonists and antagonistsActa Otolaryngol. Suppl.4795-11(1991) 2.Bertlich, M., Ihler, F., Sharaf, K., et al.Betahistine metabolites, aminoethylpyridine, and hydroxyethylpyridine increase cochlear blood flow in guinea pigs in vivoInt. J. Audiol.53(10)753-759(2014) 3.Bertlich, M., Ihler, F., Weiss, B.G., et al.Role of capillary pericytes and precapillary arterioles in the vascular mechanism of betahistine in a guinea pig inner ear modelLife Sci.18717-21(2017) 4.Lian, J., Huang, X.-F., Pai, N., et al.Ameliorating antipsychotic-induced weight gain by betahistine: Mechanisms and clinical implicationsPharmacol. Res.10651-63(2016)