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| | Biological Assay |
| Description: | To determine the effectiveness of representative compounds of this invention as histamine-3 receptor ligands (H3 receptor ligands), the following tests were conducted according to previously described methods (see Arrang J M, et al. European Journal of Pharmacology 1990; 188: 219-227; Tedford C E, et al. Journal of Pharmacology and Experimental Therapeutics 1995; 275: 598-604; Leurs R, et al. Journal of Pharmacology and Experimental Therapeutics 1996; 276: 1009-1015; and Cheng Y-C, et al. Biochemical Pharmacology 1973; 22: 3099-3108). Membrane preparations were incubated with [3H]-N-alpha-methylhistamine (0.5-1.0 nM) in the presence or absence of increasing concentrations of ligands for H3 receptor competition binding. The binding incubations were conducted in a final volume of 0.5 mL TE buffer at 25° C. and were terminated after 30 minutes. Thioperamide (30 uM) was used to define non-specific binding. All binding reactions were terminated by filtration under vacuum. |
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