Receptor preference of dynorphin A fragments in the mouse vas deferens determined by different techniques

R Schulz, M Wuster and A Herz

The opioid receptor preference of dynorphin A fragments, particularly of dynorphin A-(1-8) (DYN 8), has been evaluated in the mouse vas deferens by means of cross-tolerance studies, by their sensitivity to naloxone antagonism and by the use of the irreversible narcotic antagonist beta-funaltrexamine. The tolerance studies revealed kappa receptor activity for the longer fragments and delta activity for the shorter fragments. DYN 8 displayed kappa as well as delta activity, whereas no interaction with mu receptors was observed. The naloxone sensitivity of dynorphin A and its fragments was low with the exception of DYN 8, that displayed an intermediate sensitivity. There was no indication that this intermediate value for DYN 8 was due to an interaction with mu receptors. This conclusion was strengthened in experiments using beta-funaltrexamine. The kappa and delta activity of DYN 8 does not explain the intermediate sensitivity to naloxone. It is proposed that DYN 8 may interact in the mouse vas deferens with a different opioid receptor than the classical mu, kappa- and delta-type.

Volume 230, Issue 1, pp. 200-204, 07/01/1984
Copyright © 1984 by American Society for Pharmacology and Experimental Therapeutics