Abstract
The relative affinities for different subtypes of opioid receptors (μ, χ and δ) of the peripheral narcotic antagonist N-methyl levallorphan (SR 58002) have been studied in two in vitro smooth muscle systems (guinea-pig ileum and rabbit vas deferens) and by binding studies (guinea-pig brain and cerebellum membranes) using selective tritiated ligands. All the evidence obtained indicates that SR 58002 is a pure antagonist with relative affinity for μ receptors vs χ and δ superior to that of the parent tertiary compound, levallorphan.
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