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Use Of Lobeline Compounds In The Treatment Of Central Nervous System Diseases And Pathologies, Peter A. Crooks, Linda P. Dwoskin

Pharmaceutical Sciences Faculty Patents

Lobeline and nicotine evoke [³H]overflow from rat striatal slices preloaded with [³H]dopamine ([³H]DA). The lobeline-evoked overflow is calcium-independent and not antagonized by mecamylamine, suggesting a mechanism of action other than the stimulation of nicotinic receptors. Whereas nicotine stimulates nicotinic receptors, lobeline inhibits [³H]DA uptake into synaptic vesicles and striatal synaptosomes. The results suggest that different mechanisms are responsible for the increase in striatal DA release evoked by lobeline and nicotine. [³H]-Dihydrotetrabenazine [³H]DTBZ), used routinely to probe a high-affinity binding site-on the vesicular monoamine transporter (VMAT2) binds to vesicle …