Abstract

Administration of methionine enkephalin (ICV) to rats for 5 days resulted in the development of physical dependence as exemplified by a hypothermic response which peaked 2–8 hours after initiation of withdrawal. Twenty-four hours post-withdrawal, opioid receptor binding was determined in the striatum using a selective delta receptor ligand. These studies revealed a decreased in the number of receptors. B max decreased from 193 ± 20.4 fmoles/mg protein in controls to 136 ± 9.7 fmoles/mg protein in enkephalin treated rats. This difference is significant at p < 0.001. Existing evidence suggests that this decrease in binding is predominantly due to δ decrease in δ receptors. Hence, the present findings indicate that S receptor down-regulation in vivo may be an important mechanism in the adaptive response to chronic exposure to an endogenous opioid peptide.

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