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Overexpression of Receptors in Nonneural Human Tumors

Department of Surgery, St. Louis University, St. Louis, Missouri 63110-0250 [W. T. B., G. E. T., J. Y. M., F. E. J.]; School of Public Health [S. M. H.], St. Louis University, St. Louis, Missouri 63104; and Departments of Pathology [B. K. L.] and Biochemistry and Molecular Biology [C. J. C.], St. Louis University School of Medicine, St. Louis, Missouri 63104-1079

Previous data indicated that opioid receptors occur in both neural and nonneural human tumors. However, it has recently been shown that some of the putative opioid binding may be attributable to sites. In this study the occurrence of and opioid receptors in nonneural human tumors was assessed. The neoplasms included renal and colon carcinomas and a sarcoma. [³H]1,3-di-o-tolylguanidine was used to assay receptors by homologous competition binding assays, which when analyzed provided dissociation constant and receptor density values. Opioid binding was measured with [³H]-(-)-ethylketocyclazocine, a ligand which interacts with µ, , and subtypes. Fresh surgical specimens were obtained from 9 human neoplasms, selected for their large size, and compared with nonmalignant tissues. All 9 tumors contained sites, and dissociation constant values were within the range of 27–83 nM. Occasionally, two-site fit the data better than one-site binding, suggesting the presence of multiple sites. Opioid binding was not detected. Intratumoral variability was evaluated by sampling several locations on the periphery of the mass and one in the center. Each of the samples was bisected, with a portion reserved for histological examination to correlate morphological features with receptor data. Changes in binding were not associated with the extent of fibrosis, viability, or necrosis. Receptor density values displayed moderate intra- and intertumoral variation (coefficients of variation, 8–39 and 27–49%, respectively). More important, binding in tumors was found to be 2-fold higher than that of control nonmalignant tissue.

¹ On leave from Institute of Biostructure, Warsaw Medical School, Poland.

² To whom requests for reprints should be addressed, at Department of Surgery, The University Hospital, 3635 Vista Avenue at Grand Blvd., P.O. Box 15250, St. Louis, MO 63110-0250.

Received 7/ 9/91. Accepted 10/ 3/91.

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