Bamirastine

The binding assay is performed using 96 well microplates, and 50 mM Tris-HCl containing 0.1% BSA, pH 7.4 is used as the assay buffer. Various concentrations of test compounds (50 μL/well), [³H] pyrilamine (22 nM, 25 μL/well, final 2.75 nM) and promethazine (80 μM, 25 μL/well, non-specific binding) or equal volumes of assay buffer are mixed, and the binding assay is initiated by the addition of the membrane suspension (5 μg protein/100 μL/well). The mixtures are incubated for 1 h at room temperature and the incubation is terminated by filtration over 0.3% polyethyleneimine treated Unifilter^TM plates GF/C using a harvester. The UnifilterTM-plates are washed 3 times with 50 mM Tris-HCl buffer, pH 7.4, and dried completely. The radioactivity is counted by a TopCount system. Specific binding is defined as radioactivity bound after subtraction of nonspecific binding determined in the presence of promethazine. A K_i value (nM) is calculated, In order to characterize the inhibition of the H₁ receptor binding by Bamirastine (TAK-427), saturation curves for specific binding of [³H] pyrilamine to the membranes expressing human histamine H₁ receptors are investigated in the absence and presence of Bamirastine at 10 and 30 nM. The binding parameters are calculated from the Scatchard analysis of the saturation curves^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[1]
Male Crj: ICR mice (5 weeks old) are used. Bamirastine, Terfenadine and Epinastine in doses of 30, 100 and 300 mg/kg or vehicle (0.5% methylcellulose) are given orally. Behavior is observed for the first 2 h after drug administration.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.