Close correlations between the development of the anticonvulsant effects of diphenylhydantoin and increases in tritiated diazepam binding were observed in rats from fetal day 16 to maturation. In contrast, significant decreases in tritiated diazepam binding were observed in 2- and 3-week-old rats that were exposed in utero to diphenylhydantoin. These changes can be correlated with reported increases in seizure susceptibility after prenatal exposure to diphenylhydantoin.