A differential interaction of putative μ-selective agonists with opiate binding sites in rat brain |
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Authors: | C. Stautner, M. Wü ster, R. Schulz,A. Herz |
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Affiliation: | Department of Neuropharmacology, Max-Planck-Institut für Psychiatrie, Kraepelinstrasse 2, D-8000, München 40, Federal Republic of Germany |
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Abstract: | The availability of tritium-labelled sufentanil ([3H]SUF) allowed for a further radioligand analysis of opiate binding sites in rat brain. A comparison of the binding characteristics of [3H]SUF and [3H]dihydromorphine ([3H]DHM) revealed a very similar potency in their mutual displacement by unlabelled analogues. Furthermore, a series of putative μ-opiate agonists displayed equal potencies in displacing either [3H]SUF and [3H]DHM, the only striking exception being the highly μ-selective opioid peptide morphiceptin which was 33 times less potent in inhibiting [3H]SUF as compared to [3H]DHM binding. Additional experiments revealed further pronounced differences in [3H]SUF and [3H]DHM binding characteristics: the total amount of binding sites for [3H]SUF was 4 times higher than that for [3H]DHM and the regional distribution within particular brain areas displayed considerable differences. Furthermore, the binding of [3H]SUF was differentially modulated by sodium and GTP as compared to [3H]DHM binding. These data suggest that in rat brain, [3H]SUF interacts both with μ-opiate sites recognizing [3H]DHM and another type of opiate site, which cannot be equated with any of the, as yet, described δ- or κ-binding sites, and rather, represents a subclass of μ-opiate receptor sites. These experiments, thus, support the notion of subclasses (isoreceptors) for different types of opiate receptors. |
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