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Science 22 January 1982: Vol. 215. no. 4531, pp. 413 - 415 DOI: 10.1126/science.6120570
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Articles
Science, Vol 215, Issue 4531, 413-415
Copyright © 1982 by American Association for the Advancement of Science
Dynorphin is a specific endogenous ligand of the kappa opioid receptor
C Chavkin,
IF James,
and
A Goldstein
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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