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  • Title: Dynorphin is a specific endogenous ligand of the kappa opioid receptor.
    Author: Chavkin C, James IF, Goldstein A.
    Journal: Science; 1982 Jan 22; 215(4531):413-5. PubMed ID: 6120570.
    Abstract:
    In the guinea pig ileum myenteric plexus--longitudinal muscle preparation, dynorphin-(1--13) and the prototypical kappa agonist ethylketocyclazocine had equally poor sensitivity to naloxone antagonism and showed selective cross protection in receptor inactivation experiments with the alkylating antagonist beta-chlornaltrexamine. In binding assays with membranes from guinea pig brain, ethylketocyclazocine and dynorphin-(1--13) amide were more potent in displacing tritium-labeled ethylketocyclazocine than in displacing typical mu and delta opioid receptor ligands. In the two preparations studied, the dynorphin receptor appears to be the same as the kappa opioid receptor.
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