The effects of three formamidine pesticide or pesticide metabolites on calcium flux in the rabbit aorta were examined. U-40481 reduced the rate of both 45Ca uptake and norepinephrine (NE)-stimulated 45Ca uptake into deadventitiated rabbit aorta strips and reduced NE-stimulated efflux from 45Ca-loaded, superfused aorta strips (p less than 0.1). Neither demethylchlordimeform nor formetanate altered either 45Ca-uptake or NE-enhanced 45Ca flux. The action of U-40481 on unstimulated 45Ca uptake may result from uncoupling oxidative phosphorylation, and reduction in NE-induced 45Ca-flux may result from antagonism at NE receptors.