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[3].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Murilo B. M. de Mello, et al. Characterization and in silico Mutagenic Assessment of a New Betahistine Degradation Impurity. J. Braz. Chem. Soc. vol.30 no.7 São Paulo July 2019 Epub July 04, 2019
[2]. 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.
[3]. Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine[1]. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA)[2].
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