Abstract
Quantitative characterization of the kappa opioid receptor in the rabbit ear artery was carried out using three kappa-selective agonist compounds, dynorphin-(1-13), U-69593 and ethylketocyclazocine. Kinetic analysis was performed using the antagonist, MR 2266. Two other in vitro preparations were studied for comparison: the mouse was deferens and rabbit was deferens. To avoid mu receptor action in the mouse was deferens the irreversible mu receptor antagonist, beta-funaltrexamine, was used. It was demonstrated that, using the highly selective kappa agonist compound U-69593, Ke values for MR 2266 obtained in the three assay systems were not significantly different. These results suggest that kappa receptors present in these three tissues share identical properties.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzeneacetamides*
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Benzomorphans / pharmacology
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Cyclazocine / analogs & derivatives
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Cyclazocine / pharmacology
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Dynorphins / pharmacology
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Ethylketocyclazocine
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In Vitro Techniques
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Male
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Mice
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Muscle, Smooth, Vascular / metabolism*
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Narcotic Antagonists / pharmacology
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Peptide Fragments / pharmacology
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Pyrrolidines / pharmacology
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Rabbits
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Receptors, Opioid / metabolism*
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Receptors, Opioid, delta
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Receptors, Opioid, kappa
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Receptors, Opioid, mu
Substances
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Benzeneacetamides
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Benzomorphans
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Narcotic Antagonists
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Peptide Fragments
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Pyrrolidines
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Receptors, Opioid
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Receptors, Opioid, delta
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Receptors, Opioid, kappa
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Receptors, Opioid, mu
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MR 2266
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Ethylketocyclazocine
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dynorphin (1-13)
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Dynorphins
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U 69593
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Cyclazocine