uu.seUppsala University Publications
Change search
ReferencesLink to record
Permanent link

Direct link
Opiate modulation of dynorphin conversion in primary cultures of rat cerebral cortex
Department of Clinical Neuroscience, Experimental Alcohol and Drug Addiction Research Section, Karolinska Institute.
Show others and affiliations
1997 (English)In: Brain Research, ISSN 0006-8993, E-ISSN 1872-6240, Vol. 760, no 1-2, 85-93 p.Article in journal (Refereed) Published
Abstract [en]

Rat brain cortical cells in primary culture were used to investigate long-term effects of opiates on endopeptidases acting on dynorphin peptides. Enzyme activity in the soluble fraction of the cells converted dynorphin B to Leu-enkephalin-Arg6 and to a lesser extent to Leu-enkephalin. Five day treatment with 10 microM morphine increased the conversion to Leu-enkephalin-Arg6 by 370%. This effect was prevented by the presence of naloxone in the culture medium. The opiate-inducible activity was directed to the Arg-Arg bond in dynorphins with preference for dynorphin B > alpha-neoendorphin > > dynorphin A. The Km for the generation of Leu-enkephalin-Arg6 from dynorphin B was 40 microM. Enzyme activity was inhibited by dynorphin fragments, in the following order of potency: dynorphin A(1-13) > A(2-13) > A(1-17) > A(2-17) and by SH-reagents, suggesting the presence of a cysteine-protease. The opiate-stimulated dynorphin-converting enzyme (DCE)-activity affects the balance between dynorphin peptides (selective for kappa-opioid receptors) and enkephalin peptides (selective for delta-opioid receptors). Since both types of opioid peptides can influence the development of opiate tolerance, the change in the extent of this transformation may be functionally important.

Place, publisher, year, edition, pages
1997. Vol. 760, no 1-2, 85-93 p.
Keyword [en]
rat cerebral cortex primary culture, dynorphin, enkephalin, peptidase, mass spectrometry, morphine dependence
National Category
Medical and Health Sciences Pharmaceutical Sciences
URN: urn:nbn:se:uu:diva-50729DOI: 10.1016/S0006-8993(97)00307-7ISI: A1997XK47700012PubMedID: 9237522OAI: oai:DiVA.org:uu-50729DiVA: diva2:78638
Available from: 2008-10-17 Created: 2008-10-17 Last updated: 2011-03-10Bibliographically approved

Open Access in DiVA

No full text

Other links

Publisher's full textPubMed

Search in DiVA

By author/editor
Nylander, Ingrid
In the same journal
Brain Research
Medical and Health SciencesPharmaceutical Sciences

Search outside of DiVA

GoogleGoogle Scholar
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

Altmetric score

Total: 99 hits
ReferencesLink to record
Permanent link

Direct link