Whole-body autoradiography enables the drugs and toxicants to be distributed throughout the animal. Good results are obtained with this technique. However, certain artifacts can occur that could lead to misinterpretation, and these must be known. These artifacts are described. From the metabolic point of view, autoradiography provides data on the distribution kinetics of a compound and the elimination of radioactivity in various organs. These data are a guide for quantitative research into the metabolism of a compound. From the toxicological point of view, it must be admitted that the main purpose of this technique is to reveal the sites of retention of radioactivity. Such specific organ retention could be the consequence of the activation of a minor metabolite into a very reactive compound. If this is so, it is a specific organ effect which could not be studied by other techniques and could lead the way to a more specific organ effect which could not be studied by other techniques and could lead the way to a more appropriate line of research in the study of chronic toxicity. However, it must be recalled that the fact that a compound is retained by a specific organ does not always mean that the compound exerts a toxic effect upon the said organ. With this technique, distribution study can be performed on pregnant animals, and it provides us with more data concerning the transplacental passage of radioactive metabolites. All these aspects of the technique clearly indicate that whole-body autoradiography should be insisted upon during the early stages of development of new molecules. Successive experiments could then lead to selecting the best experimental conditions for metabolic pharmacokinetics and studies in toxicology.