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FEBS Lett. 1989 Aug 14;253(1-2):23-7.

Mu type opioid receptors in rat periaqueductal gray-enriched P2 membrane are coupled to G-protein-mediated inhibition of adenylyl cyclase.

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Department of Pharmacology, University of California, San Francisco 94143-0450.


The periaqueductal gray (PAG) region of the midbrain has been implicated in both stimulation-produced and opioid-induced analgesia. High-affinity mu-selective opioid-binding sites associated with mu type opioid receptors have been detected in rat PAG-enriched P2 membranes, and these receptors have been shown to be coupled to guanine nucleotide-binding proteins (G-proteins). In the present study the potential G-protein-mediated coupling of mu type opioid receptors to the inhibition of adenylyl cyclase was examined utilizing in vitro adenylyl cyclase assays. In the presence of Na+, opioid agonists inhibited adenylyl cyclase in a mu selective, naloxone reversible, dose dependent, and pertussis toxin sensitive manner. Overall the data suggests that mu type opioid receptors in the rat PAG are coupled to G-protein-mediated inhibition of adenylyl cyclase.

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