Gastrin is a major physiologic regulator of gastric acid secretion and growth of the oxyntic mucosa. Biologically active radiolabelled hormones may be used to characterize and localize receptors for peptide hormones. The cellular localization of the gastrin receptor in the fundic mucosa, however, is still a matter of great debate owing to difficulties in developing a gastrin receptor binding assay. Despite considerable work in several laboratories, the criteria for true receptor binding have not yet been fulfilled. The preparation of a suitable tissue receptor material (plasma membranes or isolated cells) from the heterocellular fundic mucosa seems to be the major problem. This problem may be related to the fact that the receptors are only present on the enterochromaffin-like cells (ECL), which constitute but a minor fraction of the cells in the oxyntic mucosa. Furthermore, the second messenger of gastrin is still not known, and the poor functional responsiveness of isolated cells and the oxyntic glands to gastrin further complicates the evaluation of the gastrin receptor. In this review the different steps in the gastrin receptor assay (the labelling of gastrin, preparation of the receptor, and the incubation and correlation of the binding and biologic effect of gastrin) are discussed.