Binding of Reversible and Irreversible Ligands to Rat Brain Opiate Receptors
Various lines of pharmacological and biochemical evidence support the existence of multiple opiate receptors (for review see ; also #E-2 & #NC(E)-1, this vol.) Improved binding studies with radioactive ligands of high specific activity demonstrate non-linear Scatchard plots, consistent with subpopulations of high- and low-affinity sites. Elucidation of the properties of these biochemically defined receptor subpopulations and of their correlation with opiate actions would need the development of highly selective ligands. Several attempts have been made to synthesize compounds which co-valently bind to the opiate receptor [2, 3]. Among the enkephalins the chloromethyl ketone derivative would be a likely candidate (see ).
KeywordsOpiate Receptor Scatchard Analysis Chloromethyl Ketone Unlabelled Ligand Radioactive Ligand
Unable to display preview. Download preview PDF.
- 4.Powers, J.C. (1977) in Chemistry and Biochemistry of Amino Acids, Peptides and Proteins (Weinstein, B., ed.), Dekker, New York, pp. 65–178.Google Scholar
- 6.Sziics, M., Benyhe, S., Borsodi, A., Wollemann, M., Jancsó, G., Szécsi, J. & Medzihradsky, K. (1983) Life Sci., in press.Google Scholar
- 7.Pasternak, G.W. & Snyder, S.H. (1973) Mol. Pharmacol. 10, 183–193.Google Scholar
- 8.Pasternak, G.W., Wilson, H.A. & Snyder, S.H. (1975) Mol. Pharmacol. 11, 340–351.Google Scholar
- 9.Venn, R.F. & Barnard, E.A. (1981) J. Biol. Chem. 256, 1529–1532.Google Scholar