Comparison of the binding of nicotinic agonists to receptors from human and rat cerebral cortex and from chick brain (alpha 4 beta 2) transfected into mouse fibroblasts with ion channel activity.

(-)-Nicotine, cytisine and carbachol evoked 86Rb efflux from mouse fibroblasts stably transfected with alpha 4 beta 2 chick brain nicotinic subunits. This response to (-)-nicotine was inhibited by mecamylamine and dihydro-beta-erythroidine and was mirrored by a rise in intracellular Ca2+ measured by microspectrofluorimetry. Lobeline and isoarecolone methiodide evoked no significant 86Rb from cells and unlike the above agonists displayed significantly different IC50 values for the displacement of [3H]nicotine from mammalian (rat and human cerebral cortex) and transfected fibroblast membranes.