AbstractBACKGROUND: Wheat shows selectivity to pyroxsulam, a new broad‐spectrum herbicide with high activity on blackgrass. Studies were performed to establish whether uptake, translocation or metabolism were responsible for the differential activity in wheat compared with blackgrass. In addition, the effect of the safener cloquintocet‐mexyl on metabolism was evaluated in wheat and blackgrass shoots.RESULTS: Root uptake of pyroxsulam in blackgrass was significantly higher than in wheat, suggesting a possible activity enhancement in blackgrass owing to root uptake. Translocation to foliage from root uptake as well as translocation out of treated foliage following foliar applications was low in wheat compared with blackgrass, likely owing to the rapid metabolism of pyroxsulam in wheat. Wheat metabolized pyroxsulam significantly faster than blackgrass to the less active O‐dealkylation product. Wheat shoots metabolized pyroxsulam faster when the safener cloquintocet‐mexyl was present, but cloquintocet‐mexyl did not increase the rate of metabolism in blackgrass.CONCLUSIONS: The selectivity of pyroxsulam to wheat relative to blackgrass was connected primarily with differences in the rate of metabolism and generation of an inactive metabolite. Metabolism in wheat restricted subsequent movement of radioactivity out of the treated leaf. The rapid metabolism in wheat was increased by the addition of cloquintocet‐mexyl. Copyright © 2010 Society of Chemical Industry