Profile of activity of κ receptor agonists in the rabbit vas deferens

Abstract

The purpose of this study was to investigate further the κ opioid receptor selectivity of the field-stimulated isolated rabbit vas deferens preparation and to study the profile of a series of κ agonists in this tissue. Agonists acting at μ, δ and σ receptors were without detectable effect in the rabbit vas deferens. But a number of κ agonists, including bremazocine, tifluadom, ethylketocyclazocine, ketocyclazocine, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves. Mr 2034 generally produced a shallower dose-response curve and achieved a lower maximum effect, thus acting like a partial agonist. The effect of ethylketocyclazocine was not reduced by the irreversible μ antagonist, β-funaltrexamine, confirming that it is not acting via μ receptors. Another group of drugs, including nalorphine, butorphanol and proxorphan, which produce an agonist action via κ receptors in the guinea-pig ileum and mouse vas deferens, were antagonists in the rabbit vas deferens, suggesting that this tissue will only respond to high efficacy κ agonists.