Male mice and pregnant and nonpregnant female mice were pretreated with saline or SKF 525-A (50 mg/kg, ip) and gavaged 1 hr later with [ 14C]methaqualone (MTQ) (25 mg/kg). Unchanged [ 14C]MTQ was determined in some or all of the following tissues: brain, spinal cord, eye, liver, lung, heart, spleen, kidney, muscle, fat, uterus, plasma, amniotic fluid, placenta, whole fetus, fetal brain, and liver. In saline controls, the MTQ concentrations in most adult tissues, whole fetus, and fetal brain and liver reached peak values at 1.5 hr. The tissue to plasma concentration ratios for fat and uterus were 4.5 and 1.1, respectively; those for other tissues varied from a low of 0.3 for amniotic fluid to a high of 0.8 for liver. At 1.5 hr, the fetal brain and liver contained concentrations of MTQ lower than the corresponding maternal tissues. Except for fat, the amounts in various tissues declined to trace amounts at 24 hr. Brain, plasma, lung, and liver concentrations in males and nonpregnant females were not different from each other but were significantly lower than those in pregnant mice. SKF 525-A pretreatment shifted the peak concentrations of MTQ to 3 hr in most tissues and caused marked tissue elevations.