Conversion of dynorphin-(1-9) to [Leu5]enkephalin by the mouse vas deferens in vitro.
The inhibitory action of dynorphin-(1-9) on the electrically stimulated mouse vas deferens was seen to be antagonised by the delta-selective opioid antagonist ICI 174864. The observed delta-receptor mediated responses were partially, but not totally, prevented by peptidase inhibitors which protect the C- and N-termini of dynorphin-(1-9). [3H]Dynorphin-(1-9) is rapidly degraded by slices of vasa deferentia of the mouse. The major product of this metabolism co-elutes with [Leu5]enkephalin on reverse phase HPLC. It is concluded that a major component of the inhibitory effects of dynorphin-(1-9) on the mouse vas deferens is mediated by degradation to [Leu5]enkephalin which in turn acts through delta-receptors. It is possible that in other in vitro and in vivo systems, the effects produced by dynorphin-(1-9) might be similarly mediated by delta-receptor activation.
Miller
L
L
Rance
M J
MJ
Shaw
J S
JS
Traynor
J R
JR
D000818:Animals; D001575:Benzomorphans / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D004399:Dynorphins / Q000378:metabolism*; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000378:metabolism* / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism*; D009292:Narcotic Antagonists / Q000494:pharmacology; D010446:Peptide Fragments / Q000378:metabolism*; D014649:Vas Deferens / Q000378:metabolism
D001575:Benzomorphans; D009292:Narcotic Antagonists; D010446:Peptide Fragments; C027247:MR 2266; D004743:Enkephalin, Leucine; D004399:Dynorphins; C040238:dynorphin A (1-9); C040643:N,N-diallyl-tyrosyl-alpha-aminoisobutyric acid-phenylalanyl-leucine