Determination of the sizes of the opioid receptors in their membrane environment by radiation inactivation.
Opioids, like other drugs, are thought to initiate their effects by association with their specific receptors. However, very little is known about the opioid receptor as a molecular entity. The binding components have been solubilized in detergent and purified by different approaches, but the molecular size of soluble opioid receptor complexes reported by different groups varied from 23,000 to 750,000. In this study, the technique of radiation inactivation by gamma rays was used to investigate the apparent size of the opioid receptor in rat brain membranes under different conditions. The molecular sizes of opioid receptor complexes were estimated as 313,000 +/- 13,500 in the presence of [D-Ala2, D-Leu5] enkephalin, NaCl and Gpp (NH)p; as 165,000 +/- 8,500 in the presence of NaCl only, or of both NaCl and Gpp (NH)p; as 217,000 +/- 6,600 in the presence of Gpp (NH)p only; and as 286,000 +/- 60,900 in the presence of MgCl2 only. A simple model has been proposed to explain these different apparent target sizes of opioid receptors obtained under different conditions.
D000818:Animals; D001923:Brain Chemistry; D002462:Cell Membrane / Q000032:analysis* / Q000528:radiation effects / Q000648:ultrastructure; D004307:Dose-Response Relationship, Radiation; D005720:Gamma Rays; D008297:Male; D008970:Molecular Weight; D011485:Protein Binding / Q000528:radiation effects; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000032:analysis* / Q000528:radiation effects
D011957:Receptors, Opioid